CN103328487B - 作为pde10a酶抑制剂的咪唑衍生物 - Google Patents

作为pde10a酶抑制剂的咪唑衍生物 Download PDF

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Publication number
CN103328487B
CN103328487B CN201180065325.2A CN201180065325A CN103328487B CN 103328487 B CN103328487 B CN 103328487B CN 201180065325 A CN201180065325 A CN 201180065325A CN 103328487 B CN103328487 B CN 103328487B
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China
Prior art keywords
triazolo
imidazo
compound
dimethyl
isoindole
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Expired - Fee Related
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CN201180065325.2A
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English (en)
Chinese (zh)
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CN103328487A (zh
Inventor
J.科勒
J.尼伊森
M.马里戈
J.P.基尔布恩
M.兰格尔德
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H Lundbeck AS
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H Lundbeck AS
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    • 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
    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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

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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)
CN201180065325.2A 2010-11-19 2011-11-18 作为pde10a酶抑制剂的咪唑衍生物 Expired - Fee Related CN103328487B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201001045 2010-11-19
DKPA201001045 2010-11-19
PCT/DK2011/000136 WO2012065612A1 (en) 2010-11-19 2011-11-18 Imidazole derivatives as pde10a enzyme inhibitors

Publications (2)

Publication Number Publication Date
CN103328487A CN103328487A (zh) 2013-09-25
CN103328487B true CN103328487B (zh) 2015-11-25

Family

ID=45217102

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180065325.2A Expired - Fee Related CN103328487B (zh) 2010-11-19 2011-11-18 作为pde10a酶抑制剂的咪唑衍生物

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Country Link
EP (1) EP2640731B9 (enExample)
JP (1) JP5937608B2 (enExample)
KR (1) KR101916487B1 (enExample)
CN (1) CN103328487B (enExample)
AP (1) AP3342A (enExample)
AR (1) AR083926A1 (enExample)
AU (1) AU2011331607B2 (enExample)
BR (1) BR112013012378A2 (enExample)
CA (1) CA2817663C (enExample)
CR (1) CR20130226A (enExample)
DK (1) DK2640731T3 (enExample)
EA (1) EA027082B1 (enExample)
EC (1) ECSP13012698A (enExample)
ES (1) ES2547090T3 (enExample)
GE (1) GEP20156346B (enExample)
GT (1) GT201300130A (enExample)
HU (1) HUE025596T2 (enExample)
JO (1) JO3089B1 (enExample)
ME (1) ME02193B (enExample)
MY (1) MY163327A (enExample)
NZ (1) NZ610353A (enExample)
PE (1) PE20141534A1 (enExample)
PH (1) PH12013500968A1 (enExample)
PL (1) PL2640731T3 (enExample)
PT (1) PT2640731E (enExample)
RS (1) RS54210B1 (enExample)
SG (1) SG190282A1 (enExample)
SI (1) SI2640731T1 (enExample)
TW (1) TWI541245B (enExample)
UA (1) UA112065C2 (enExample)
WO (1) WO2012065612A1 (enExample)
ZA (1) ZA201303607B (enExample)

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
JP6106603B2 (ja) * 2011-01-11 2017-04-05 スノビオン プハルマセウトイカルス インコーポレイテッド ヘテロアリール化合物及びその使用方法
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
WO2013192273A1 (en) * 2012-06-19 2013-12-27 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
US10633382B2 (en) 2016-10-18 2020-04-28 H. Lundbeck A/S Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as PDE1 inhibitors
LT3532064T (lt) 2016-10-28 2020-09-25 H. Lundbeck A/S Kompleksiniai gydymai, apimantys imidazopirazonus, skirti psichiatrinių ir (arba) kognityvinių sutrikimų gydymui
RU2019108717A (ru) 2016-10-28 2020-11-30 Х. Лундбекк А/С Комбинированные средства для лечения, предусматривающего введение имидазопиразинонов
WO2020094591A1 (en) 2018-11-06 2020-05-14 H. Lundbeck A/S Pde10a inhibitors for treating negative symptoms and cognitive impairments in a patient suffering from schizophrenia
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009152825A1 (en) * 2008-06-20 2009-12-23 H. Lundbeck A/S Novel phenylimidazole derivatives as pde10a enzyme inhibitors
WO2010145668A1 (en) * 2009-06-19 2010-12-23 H. Lundbeck A/S Novel phenylimidazole derivative as pde10a enzyme inhibitor
WO2011072695A1 (en) * 2009-12-17 2011-06-23 H. Lundbeck A/S Phenylimidazole derivatives comprising an ethynylene linker as pde10a enzyme inhibitors
WO2011072694A1 (en) * 2009-12-17 2011-06-23 H. Lundbeck A/S Heteroaromatic phenylimidazole derivatives as pde10a enzyme inhibitors

Family Cites Families (13)

* 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
IL149106A0 (en) 2001-04-20 2002-11-10 Pfizer Prod Inc Therapeutic use of selective pde10 inhibitors
US20030032579A1 (en) 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
EP1641457B1 (en) 2003-06-30 2009-08-05 Nycomed GmbH Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors
MXPA05013553A (es) 2003-06-30 2006-03-09 Altana Pharma Ag Pirrolodihidroisoquinolinas como inhibidores de pde10.
EP1651251A4 (en) 2003-07-31 2008-06-18 Bayer Pharmaceuticals Corp METHOD FOR THE TREATMENT OF DIABETES AND RELATED DISEASES USING PDE 10A INHIBITORS
EP1723134A2 (en) 2004-02-18 2006-11-22 Pfizer Products Incorporated Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
BRPI0511854A (pt) 2004-06-07 2008-01-15 Pfizer Prod Inc inibição de fosfodiestearase 10 como tratamento para condições relacionados com a obesidade e relacionadas a sìndrome metabólica
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
CA2578996A1 (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
US8133897B2 (en) * 2008-06-20 2012-03-13 H. Lundbeck A/S Phenylimidazole derivatives 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009152825A1 (en) * 2008-06-20 2009-12-23 H. Lundbeck A/S Novel phenylimidazole derivatives as pde10a enzyme inhibitors
WO2010145668A1 (en) * 2009-06-19 2010-12-23 H. Lundbeck A/S Novel phenylimidazole derivative as pde10a enzyme inhibitor
WO2011072695A1 (en) * 2009-12-17 2011-06-23 H. Lundbeck A/S Phenylimidazole derivatives comprising an ethynylene linker as pde10a enzyme inhibitors
WO2011072694A1 (en) * 2009-12-17 2011-06-23 H. Lundbeck A/S Heteroaromatic phenylimidazole derivatives as pde10a enzyme inhibitors

Also Published As

Publication number Publication date
MY163327A (en) 2017-09-15
AR083926A1 (es) 2013-04-10
EP2640731A1 (en) 2013-09-25
BR112013012378A2 (pt) 2016-08-30
AU2011331607B2 (en) 2016-05-19
SG190282A1 (en) 2013-06-28
DK2640731T3 (en) 2015-08-31
AP3342A (en) 2015-07-31
ECSP13012698A (es) 2013-08-30
WO2012065612A1 (en) 2012-05-24
ZA201303607B (en) 2014-07-30
PE20141534A1 (es) 2014-11-16
KR101916487B1 (ko) 2018-11-07
CN103328487A (zh) 2013-09-25
ME02193B (me) 2016-02-20
PT2640731E (pt) 2015-10-13
PL2640731T3 (pl) 2015-11-30
HUE025596T2 (en) 2016-03-29
TWI541245B (zh) 2016-07-11
CA2817663A1 (en) 2012-05-24
KR20140009192A (ko) 2014-01-22
TW201300391A (zh) 2013-01-01
GT201300130A (es) 2015-01-16
AU2011331607A1 (en) 2013-05-30
ES2547090T3 (es) 2015-10-01
EA201390741A1 (ru) 2013-11-29
NZ610353A (en) 2015-01-30
JO3089B1 (ar) 2017-03-15
AP2013006928A0 (en) 2013-06-30
CR20130226A (es) 2013-09-03
GEP20156346B (en) 2015-08-10
JP5937608B2 (ja) 2016-06-22
PH12013500968A1 (en) 2022-10-24
UA112065C2 (uk) 2016-07-25
EP2640731B9 (en) 2015-11-25
SI2640731T1 (sl) 2015-10-30
EP2640731B1 (en) 2015-07-08
RS54210B1 (sr) 2015-12-31
EA027082B1 (ru) 2017-06-30
CA2817663C (en) 2020-04-28
JP2013542963A (ja) 2013-11-28

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Granted publication date: 20151125

Termination date: 20211118