CN104619344A - 治疗阿尔茨海默病的方法及其药物组合物 - Google Patents

治疗阿尔茨海默病的方法及其药物组合物 Download PDF

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Publication number
CN104619344A
CN104619344A CN201380046768.6A CN201380046768A CN104619344A CN 104619344 A CN104619344 A CN 104619344A CN 201380046768 A CN201380046768 A CN 201380046768A CN 104619344 A CN104619344 A CN 104619344A
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China
Prior art keywords
compound
fluoro
indol
ethyl
propoxyl group
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Pending
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CN201380046768.6A
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English (en)
Chinese (zh)
Inventor
E·施密特
J·阿伯格
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H Lundbeck AS
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H Lundbeck AS
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Application filed by H Lundbeck AS filed Critical H Lundbeck AS
Publication of CN104619344A publication Critical patent/CN104619344A/zh
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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380046768.6A 2012-09-09 2013-09-06 治疗阿尔茨海默病的方法及其药物组合物 Pending CN104619344A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261698664P 2012-09-09 2012-09-09
US61/698,664 2012-09-09
US201361782084P 2013-03-14 2013-03-14
US61/782,084 2013-03-14
PCT/EP2013/068516 WO2014037532A1 (en) 2012-09-09 2013-09-06 Methods of treating alzheimer's disease and pharmaceutical compositions thereof

Publications (1)

Publication Number Publication Date
CN104619344A true CN104619344A (zh) 2015-05-13

Family

ID=49118521

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380046768.6A Pending CN104619344A (zh) 2012-09-09 2013-09-06 治疗阿尔茨海默病的方法及其药物组合物

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Country Link
US (4) US9375418B2 (https=)
EP (1) EP2892563B1 (https=)
JP (2) JP6693744B2 (https=)
KR (2) KR102342127B1 (https=)
CN (1) CN104619344A (https=)
AP (1) AP2015008306A0 (https=)
AU (1) AU2013311573B2 (https=)
BR (1) BR112015005117B1 (https=)
CA (1) CA2883751C (https=)
CL (1) CL2015000578A1 (https=)
CY (1) CY1121062T1 (https=)
DK (1) DK2892563T3 (https=)
EA (1) EA030448B1 (https=)
ES (1) ES2703630T3 (https=)
GE (1) GEP201706776B (https=)
HR (1) HRP20182069T1 (https=)
IL (1) IL237369B (https=)
JO (1) JO3459B1 (https=)
LT (1) LT2892563T (https=)
MX (1) MX368305B (https=)
MY (1) MY182539A (https=)
NI (1) NI201500031A (https=)
NZ (1) NZ630589A (https=)
PL (1) PL2892563T3 (https=)
PT (1) PT2892563T (https=)
RS (1) RS58104B1 (https=)
RU (1) RU2675786C2 (https=)
SG (1) SG11201501774QA (https=)
SI (1) SI2892563T1 (https=)
SM (1) SMT201800678T1 (https=)
TN (1) TN2015000076A1 (https=)
TW (1) TWI632909B (https=)
WO (1) WO2014037532A1 (https=)

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CN106309436A (zh) * 2016-07-25 2017-01-11 宁波大学 可用作乙酰胆碱酯酶抑制剂的色胺衍生物及其用途
CN107118146A (zh) * 2017-04-13 2017-09-01 宁波大学 一种6‑溴色胺衍生物及其制备方法和用途
CN109069650A (zh) * 2016-04-26 2018-12-21 H.隆德贝克有限公司 乙酰胆碱酯酶抑制剂和艾达鲁吡啶用于减少帕金森氏病患者跌倒的用途
CN109069466A (zh) * 2016-05-11 2018-12-21 H.隆德贝克有限公司 5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病

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EP2508177A1 (en) 2007-12-12 2012-10-10 Glaxo Group Limited Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
US9126946B2 (en) 2008-10-28 2015-09-08 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
JO3459B1 (ar) 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
US9604982B2 (en) 2013-03-14 2017-03-28 Janssen Pharmaceutica Nv P2X7 modulators
TWI644671B (zh) 2013-03-14 2018-12-21 比利時商健生藥品公司 P2x7調節劑
US9040534B2 (en) 2013-03-14 2015-05-26 Janssen Pharmaceutica Nv [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
ES2845473T3 (es) 2013-03-14 2021-07-26 Boehringer Ingelheim Int (Bencil-ciano-metil)-amidas sustituidas de ácido 2-aza-biciclo[2.2.1]heptano-3-carboxílico inhibidores de la catepsina- C
JO3639B1 (ar) 2014-07-04 2020-08-27 H Lundbeck As صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد
EP3511331A1 (en) 2014-09-12 2019-07-17 Boehringer Ingelheim International GmbH Spirocyclic inhibitors of cathepsin c
WO2016039977A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulators
AU2015315693B2 (en) 2014-09-12 2020-01-16 Janssen Pharmaceutica Nv P2X7 modulating n-acyl-triazolopyrazines
CN105175307A (zh) * 2014-11-18 2015-12-23 苏州晶云药物科技有限公司 Lu AE58054的盐酸盐晶型A及其制备方法和用途
JP2018515607A (ja) * 2015-05-07 2018-06-14 アクソファント サイエンシーズ ゲーエムベーハーAxovant Sciences Gmbh 神経変性疾患を処置する組成物および方法
US10022355B2 (en) 2015-06-12 2018-07-17 Axovant Sciences Gmbh Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of REM sleep behavior disorder
BR112018000728A2 (pt) 2015-07-15 2018-09-04 Axovant Sciences Gmbh resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo
EA036347B1 (ru) 2016-05-18 2020-10-29 Сувен Лайф Сайенсиз Лимитед Комбинация чистых антагонистов 5-ht6 рецепторов с ингибиторами ацетилхолинэстеразы
BR112019001145A2 (pt) * 2017-05-24 2019-04-30 H. Lundbeck A/S combinação de um antagonista do receptor 5-ht6 e de um inibidor de acetilcolinesterase para uso no tratamento da doença de alzheimer em uma subpopulação de pacientes portadores de alelos de apoe4
MY205440A (en) 2018-09-28 2024-10-21 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
KR20210069079A (ko) 2018-09-28 2021-06-10 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 조절제
JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ.ベー. 放射線標識されたmgl petリガンド
NL2024431B1 (en) 2019-12-11 2021-09-07 Sulfateq Bv Compounds for treatment of alzheimer’s disease
BR112022019077A2 (pt) 2020-03-26 2022-12-27 Janssen Pharmaceutica Nv Moduladores da monoacilglicerol lipase
EP3960174B1 (en) 2020-08-28 2024-10-30 Westfälische Wilhelms-Universität Münster Parasympathetic active phenyl-glycosid-substituted hydroxy-methyl-piperidine and -pyrrolidine alkaloids for medicinal use
WO2025198622A1 (en) * 2024-03-22 2025-09-25 Queen Aaric Magnesium and lidocaine composition

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109069650A (zh) * 2016-04-26 2018-12-21 H.隆德贝克有限公司 乙酰胆碱酯酶抑制剂和艾达鲁吡啶用于减少帕金森氏病患者跌倒的用途
CN109069466A (zh) * 2016-05-11 2018-12-21 H.隆德贝克有限公司 5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病
CN109069466B (zh) * 2016-05-11 2021-06-15 H.隆德贝克有限公司 5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病
CN106309436A (zh) * 2016-07-25 2017-01-11 宁波大学 可用作乙酰胆碱酯酶抑制剂的色胺衍生物及其用途
CN107118146A (zh) * 2017-04-13 2017-09-01 宁波大学 一种6‑溴色胺衍生物及其制备方法和用途
CN107118146B (zh) * 2017-04-13 2019-09-03 宁波大学 一种6-溴色胺衍生物及其制备方法和用途

Also Published As

Publication number Publication date
BR112015005117A2 (pt) 2017-07-04
IL237369B (en) 2018-11-29
SG11201501774QA (en) 2015-05-28
MX2015002879A (es) 2015-07-06
CA2883751A1 (en) 2014-03-13
US20160256437A1 (en) 2016-09-08
AU2013311573B2 (en) 2017-10-12
BR112015005117B1 (pt) 2022-06-21
WO2014037532A1 (en) 2014-03-13
AU2013311573A1 (en) 2015-03-12
RU2675786C2 (ru) 2018-12-25
TW201414474A (zh) 2014-04-16
US10660878B2 (en) 2020-05-26
CY1121062T1 (el) 2019-12-11
TN2015000076A1 (en) 2016-06-29
KR20150065680A (ko) 2015-06-15
US20180071254A1 (en) 2018-03-15
DK2892563T3 (en) 2019-01-21
RS58104B1 (sr) 2019-02-28
SI2892563T1 (sl) 2019-02-28
NI201500031A (es) 2016-02-15
JP2019059760A (ja) 2019-04-18
CA2883751C (en) 2020-11-24
US9687473B2 (en) 2017-06-27
JP6693744B2 (ja) 2020-05-13
AU2013311573A8 (en) 2015-03-19
HK1212217A1 (en) 2016-06-10
AP2015008306A0 (en) 2015-03-31
LT2892563T (lt) 2019-01-10
EP2892563B1 (en) 2018-11-14
MY182539A (en) 2021-01-25
CL2015000578A1 (es) 2015-05-15
US20160354343A1 (en) 2016-12-08
KR102342127B1 (ko) 2021-12-21
NZ630589A (en) 2015-12-24
KR20200137028A (ko) 2020-12-08
US9375418B2 (en) 2016-06-28
IL237369A0 (en) 2015-04-30
EA201590353A1 (ru) 2016-03-31
EA030448B1 (ru) 2018-08-31
US9789085B2 (en) 2017-10-17
RU2015107877A (ru) 2016-10-27
MX368305B (es) 2019-09-27
JO3459B1 (ar) 2020-07-05
GEP201706776B (en) 2017-11-27
HRP20182069T1 (hr) 2019-02-08
PL2892563T3 (pl) 2019-04-30
PT2892563T (pt) 2019-01-10
SMT201800678T1 (it) 2019-02-28
TWI632909B (zh) 2018-08-21
EP2892563A1 (en) 2015-07-15
US20140073681A1 (en) 2014-03-13
JP2015528471A (ja) 2015-09-28
ES2703630T3 (es) 2019-03-11

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Application publication date: 20150513