TWI541245B - 作為pde10a酵素抑制劑的咪唑衍生物 - Google Patents

作為pde10a酵素抑制劑的咪唑衍生物 Download PDF

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Publication number
TWI541245B
TWI541245B TW100141570A TW100141570A TWI541245B TW I541245 B TWI541245 B TW I541245B TW 100141570 A TW100141570 A TW 100141570A TW 100141570 A TW100141570 A TW 100141570A TW I541245 B TWI541245 B TW I541245B
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TW
Taiwan
Prior art keywords
group
triazolo
compound
imidazo
dimethyl
Prior art date
Application number
TW100141570A
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English (en)
Chinese (zh)
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TW201300391A (zh
Inventor
洋 凱爾勒
傑寇 尼爾森
莫羅 瑪莉格
約翰 保羅 琪爾伯
摩頓 藍格德
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H 朗德貝克公司
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Publication of TW201300391A publication Critical patent/TW201300391A/zh
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Publication of TWI541245B publication Critical patent/TWI541245B/zh

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    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (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)
TW100141570A 2010-11-19 2011-11-15 作為pde10a酵素抑制劑的咪唑衍生物 TWI541245B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA201001045 2010-11-19

Publications (2)

Publication Number Publication Date
TW201300391A TW201300391A (zh) 2013-01-01
TWI541245B true TWI541245B (zh) 2016-07-11

Family

ID=45217102

Family Applications (1)

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TW100141570A TWI541245B (zh) 2010-11-19 2011-11-15 作為pde10a酵素抑制劑的咪唑衍生物

Country Status (31)

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EP (1) EP2640731B9 (US20070167479A1-20070719-C00034.png)
JP (1) JP5937608B2 (US20070167479A1-20070719-C00034.png)
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SI (1) SI2640731T1 (US20070167479A1-20070719-C00034.png)
TW (1) TWI541245B (US20070167479A1-20070719-C00034.png)
UA (1) UA112065C2 (US20070167479A1-20070719-C00034.png)
WO (1) WO2012065612A1 (US20070167479A1-20070719-C00034.png)
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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8552045B2 (en) 2010-11-19 2013-10-08 H. Lundbeck A/S Tricyclic imidazole compounds as PDE10 inhibitors
EP3210984B1 (en) 2011-01-11 2019-06-19 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
WO2013045607A1 (en) * 2011-09-30 2013-04-04 H. Lundbeck A/S Quinazoline linked heteroaromatic tricycle derivatives as pde10a enzyme inhibitors
WO2013107856A1 (en) * 2012-01-20 2013-07-25 H. Lundbeck A/S Imidazole derivatives as pde10a enzyme inhibitors
NZ702239A (en) 2012-06-19 2017-01-27 Sunovion Pharmaceuticals Inc Heteroaryl compounds and methods of use thereof
CN103435617B (zh) * 2013-08-22 2016-04-27 南京华安药业有限公司 一种6,7-二氢-5H-吡咯并[1,2-a]咪唑-2-甲醛的合成方法
JO3627B1 (ar) 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
TWI729109B (zh) 2016-04-12 2021-06-01 丹麥商H 朗德貝克公司 作爲PDE1抑制劑的1,5-二氫-4H-吡唑并[3,4-d]嘧啶-4-酮和1,5-二氫-4H-吡唑并[4,3-c]吡啶-4-酮
CN109843884B (zh) 2016-10-18 2022-03-04 H.隆德贝克有限公司 作为pde1抑制剂的咪唑并吡嗪酮、吡唑并嘧啶酮和吡唑并吡啶酮
CA3041595A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising administration of imidazopyrazinones
EP3532064B1 (en) 2016-10-28 2020-07-29 H. Lundbeck A/S Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
TW202031250A (zh) 2018-11-06 2020-09-01 丹麥商H 朗德貝克公司 用於治療負性症狀和認知損傷之pde10a抑制劑
CN109776527A (zh) * 2019-02-21 2019-05-21 药雅科技(上海)有限公司 一种5-溴-7-氮杂吲哚的合成方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8307865D0 (en) 1983-03-22 1983-04-27 Fujisawa Pharmaceutical Co Benzimidazole derivatives
US5571775A (en) 1994-07-11 1996-11-05 Dowelanco N-aryl[1,2,4]triazolo[1,5-a]pyridine-2-sulfonamide herbicides
US20030032579A1 (en) 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
IL149106A0 (en) 2001-04-20 2002-11-10 Pfizer Prod Inc Therapeutic use of selective pde10 inhibitors
UA86591C2 (ru) 2003-06-30 2009-05-12 Алтана Фарма Аг Пирролодигидроизохинолины как ингибиторы pde10, фармацевтическая композиция на их основе
CA2530114A1 (en) 2003-06-30 2005-01-13 Altana Pharma Ag Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors
WO2005012485A2 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
WO2005082883A2 (en) 2004-02-18 2005-09-09 Pfizer Products Inc. Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
CA2568929A1 (en) 2004-06-07 2005-12-22 Pfizer Products Inc. Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
WO2006028957A1 (en) 2004-09-03 2006-03-16 Memory Pharmaceuticals Corporation 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms
TWI501965B (zh) * 2008-06-20 2015-10-01 Lundbeck & Co As H 作為pde10a酵素抑制劑之新穎苯基咪唑衍生物
UA102693C2 (ru) * 2008-06-20 2013-08-12 Х. Луннбек А/С Производные фенилимидазола как ингибиторы фермента pde10a
US8133897B2 (en) * 2008-06-20 2012-03-13 H. Lundbeck A/S Phenylimidazole derivatives as PDE10A enzyme inhibitors
TW201200516A (en) * 2009-12-17 2012-01-01 Lundbeck & Co As H Phenylimidazole derivatives comprising an ethynylene linker as PDE10A enzyme inhibitors
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
TWI485151B (zh) * 2009-12-17 2015-05-21 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族苯基咪唑衍生物

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Publication number Publication date
AU2011331607B2 (en) 2016-05-19
CA2817663A1 (en) 2012-05-24
RS54210B1 (en) 2015-12-31
BR112013012378A2 (pt) 2016-08-30
SG190282A1 (en) 2013-06-28
ECSP13012698A (es) 2013-08-30
WO2012065612A1 (en) 2012-05-24
EP2640731A1 (en) 2013-09-25
PT2640731E (pt) 2015-10-13
EA027082B1 (ru) 2017-06-30
CN103328487A (zh) 2013-09-25
AP2013006928A0 (en) 2013-06-30
KR101916487B1 (ko) 2018-11-07
GEP20156346B (en) 2015-08-10
MY163327A (en) 2017-09-15
ME02193B (me) 2016-02-20
AR083926A1 (es) 2013-04-10
CN103328487B (zh) 2015-11-25
ZA201303607B (en) 2014-07-30
EA201390741A1 (ru) 2013-11-29
GT201300130A (es) 2015-01-16
HUE025596T2 (en) 2016-03-29
CR20130226A (es) 2013-09-03
JP5937608B2 (ja) 2016-06-22
TW201300391A (zh) 2013-01-01
EP2640731B1 (en) 2015-07-08
AU2011331607A1 (en) 2013-05-30
JP2013542963A (ja) 2013-11-28
SI2640731T1 (sl) 2015-10-30
DK2640731T3 (en) 2015-08-31
ES2547090T3 (es) 2015-10-01
PL2640731T3 (pl) 2015-11-30
PE20141534A1 (es) 2014-11-16
NZ610353A (en) 2015-01-30
UA112065C2 (uk) 2016-07-25
EP2640731B9 (en) 2015-11-25
AP3342A (en) 2015-07-31
JO3089B1 (ar) 2017-03-15
CA2817663C (en) 2020-04-28
KR20140009192A (ko) 2014-01-22

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