EA201390353A1 - Производное пиразолохинолина - Google Patents

Производное пиразолохинолина

Info

Publication number
EA201390353A1
EA201390353A1 EA201390353A EA201390353A EA201390353A1 EA 201390353 A1 EA201390353 A1 EA 201390353A1 EA 201390353 A EA201390353 A EA 201390353A EA 201390353 A EA201390353 A EA 201390353A EA 201390353 A1 EA201390353 A1 EA 201390353A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bladder
diseases
pde9
derivative
impaired
Prior art date
Application number
EA201390353A
Other languages
English (en)
Other versions
EA023493B1 (ru
Inventor
Хироюки Каизава
Хирофуми Ямамото
Кадзунори Камидзо
Мари Сугита
Рюси Сео
Сатоси Ямамото
Ацуси Укай
Original Assignee
Астеллас Фарма Инк.
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 Астеллас Фарма Инк. filed Critical Астеллас Фарма Инк.
Publication of EA201390353A1 publication Critical patent/EA201390353A1/ru
Publication of EA023493B1 publication Critical patent/EA023493B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D487/02—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 two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07D487/02—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 two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Предложено соединение, которое обладает PDE9-ингибирующей активностью и является применимым в качестве активного ингредиента средства для лечения и/или предотвращения нарушения накопительной функции мочевого пузыря, нарушения мочеиспускания, заболеваний мочевого пузыря/уретральных заболеваний и тому подобного. Авторы исследовали соединение, которое обладает PDE9-ингибирующим действием и является применимым в качестве активного ингредиента средства для лечения и/или предотвращения нарушения накопительной функции мочевого пузыря, нарушения мочеиспускания, заболеваний мочевого пузыря/уретральных заболеваний и тому подобного, и таким образом обнаружили, что производное пиразолохинолина обладает PDE9-ингибирующим действием, тем самым завершив настоящее изобретение. Производное пиразолохинолина настоящего изобретения обладает PDE9-ингибирующим действием и его можно применять в качестве агента для предотвращения и/или лечения нарушения накопительной функции мочевого пузыря, нарушения мочеиспускания, заболеваний мочевого пузыря/уретральных заболеваний и тому подобного.
EA201390353A 2010-09-07 2011-09-07 Производное пиразолохинолина EA023493B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2010200403 2010-09-07
PCT/JP2011/070410 WO2012033144A1 (ja) 2010-09-07 2011-09-07 ピラゾロキノリン化合物

Publications (2)

Publication Number Publication Date
EA201390353A1 true EA201390353A1 (ru) 2013-08-30
EA023493B1 EA023493B1 (ru) 2016-06-30

Family

ID=45810740

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390353A EA023493B1 (ru) 2010-09-07 2011-09-07 Производное пиразолохинолина

Country Status (18)

Country Link
US (1) US8822448B2 (ru)
EP (1) EP2615089B1 (ru)
JP (1) JP5888237B2 (ru)
KR (1) KR101860583B1 (ru)
CN (1) CN103097383B (ru)
BR (1) BR112013005444B1 (ru)
CA (1) CA2810696C (ru)
CY (1) CY1117547T1 (ru)
DK (1) DK2615089T3 (ru)
EA (1) EA023493B1 (ru)
ES (1) ES2583528T3 (ru)
HR (1) HRP20160473T1 (ru)
HU (1) HUE028038T2 (ru)
MX (1) MX2013002584A (ru)
PL (1) PL2615089T3 (ru)
RS (1) RS54834B1 (ru)
SI (1) SI2615089T1 (ru)
WO (1) WO2012033144A1 (ru)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9169246B2 (en) * 2011-09-26 2015-10-27 Sanofi Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof
EP2573073B1 (en) * 2011-09-26 2014-10-22 Sanofi Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof
JP6042060B2 (ja) * 2011-09-26 2016-12-14 サノフイ ピラゾロキノリノン誘導体、その調製および治療上の使用
CN103930423B (zh) * 2011-10-07 2015-09-16 卫材Rd管理有限公司 吡唑并喹啉衍生物
CN102786525B (zh) 2012-08-08 2014-12-17 中山大学 N-取代吡唑并[3,4-d]嘧啶酮类化合物、其制备方法及其应用
RU2655171C2 (ru) * 2013-04-05 2018-05-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Соль производного пиразолохинолина и ее кристалл
CA2904820C (en) * 2013-04-05 2021-05-18 Eisai R&D Management Co., Ltd. Pyridinylpyrazoloquinoline compound
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
AR102849A1 (es) * 2015-03-09 2017-03-29 Astellas Pharma Inc Compuesto de piridina bicíclica
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AU2018278422B2 (en) 2017-06-01 2022-03-17 Eisai R&D Management Co., Ltd. Lewy body disease therapeutic agent containing pyrazoloquinoline derivative
BR112019023557A2 (pt) 2017-06-01 2020-06-02 Eisai R&D Management Co., Ltd. Composição farmacêutica compreendendo inibidor de pde9
US11147803B2 (en) 2017-06-01 2021-10-19 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine
US11833146B2 (en) 2017-06-01 2023-12-05 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil
KR20240101561A (ko) 2021-10-14 2024-07-02 인사이트 코포레이션 Kras의 저해제로서의 퀴놀린 화합물
AU2023235233A1 (en) 2022-03-14 2024-09-12 Slap Pharmaceuticals Llc Multicyclic compounds

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5192768A (en) 1990-09-14 1993-03-09 Kyowa Hakko Kogyo Co., Ltd. Pyrazoloquinoline derivatives
JPH05132484A (ja) * 1991-04-26 1993-05-28 Otsuka Pharmaceut Factory Inc ピラゾロキノリン及びピラゾロナフチリジン誘導体
HN2002000317A (es) 2001-11-02 2003-05-21 Pfizer Inhibidores de pde9 para tratamiento de trastornos cardiovasculares
IL161155A0 (en) 2001-11-02 2004-08-31 Pfizer Prod Inc Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
PL378245A1 (pl) 2003-01-09 2006-03-20 Astellas Pharma Inc. Pochodne pirolopirydazyny
TW200508233A (en) 2003-05-29 2005-03-01 Millennium Pharm Inc Chk-1 inhibitors
JP2006045118A (ja) * 2004-08-04 2006-02-16 Mochida Pharmaceut Co Ltd 新規ピラゾロキノロン誘導体
US8293754B2 (en) 2005-06-14 2012-10-23 Aska Pharmaceutical Co., Ltd. Thienopyrimidine derivatives
US7671069B2 (en) 2006-03-30 2010-03-02 Chemocentryx, Inc. Tricyclic, heteroaromatic compounds modulating CXCR4 and/ or CXCR7
WO2008018306A1 (fr) 2006-08-08 2008-02-14 Aska Pharmaceutical Co., Ltd. Dérivé quinazoline
KR101563103B1 (ko) * 2006-12-13 2015-10-23 아스카 세이야쿠 가부시키가이샤 퀴녹살린 유도체
AU2007332439A1 (en) * 2006-12-13 2008-06-19 Aska Pharmaceutical Co., Ltd. Therapeutic agent for urinary tract disease
NZ580904A (en) 2007-05-11 2012-02-24 Pfizer Amino-heterocyclic compounds for inhibiting pde9
CA2706018C (en) 2007-11-30 2015-11-24 Boehringer Ingelheim International Gmbh 1, 5-dihydro-pyrazolo [3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators for the treatment of cns disorders
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
PE20110383A1 (es) 2008-09-08 2011-07-15 Boehringer Ingelheim Int Pirazolopirimidinonas como inhibidores de la fosfodiesterasa 9a (pde9a)
US9259564B2 (en) 2009-01-22 2016-02-16 Avent, Inc. Enteral feeding assembly with lock assembly
TWI404721B (zh) 2009-01-26 2013-08-11 Pfizer 胺基－雜環化合物

Also Published As

Publication number Publication date
EP2615089A4 (en) 2014-01-01
EA023493B1 (ru) 2016-06-30
EP2615089A1 (en) 2013-07-17
BR112013005444B1 (pt) 2019-07-09
SI2615089T1 (sl) 2016-08-31
JP5888237B2 (ja) 2016-03-16
CA2810696C (en) 2018-09-18
US20130225553A1 (en) 2013-08-29
HUE028038T2 (en) 2016-11-28
KR101860583B1 (ko) 2018-05-23
BR112013005444A2 (pt) 2017-09-19
EP2615089B1 (en) 2016-04-27
CA2810696A1 (en) 2012-03-15
KR20130106358A (ko) 2013-09-27
WO2012033144A1 (ja) 2012-03-15
CN103097383B (zh) 2015-09-16
RS54834B1 (sr) 2016-10-31
MX2013002584A (es) 2013-04-29
DK2615089T3 (en) 2016-06-06
CY1117547T1 (el) 2017-04-26
CN103097383A (zh) 2013-05-08
PL2615089T3 (pl) 2016-10-31
HRP20160473T1 (hr) 2016-07-29
ES2583528T3 (es) 2016-09-21
JPWO2012033144A1 (ja) 2014-01-20
US8822448B2 (en) 2014-09-02

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM