CA2450167A1 - Macrocycles useful in the treatment of alzheimer's disease - Google Patents

Macrocycles useful in the treatment of alzheimer's disease Download PDF

Info

Publication number
CA2450167A1
CA2450167A1 CA002450167A CA2450167A CA2450167A1 CA 2450167 A1 CA2450167 A1 CA 2450167A1 CA 002450167 A CA002450167 A CA 002450167A CA 2450167 A CA2450167 A CA 2450167A CA 2450167 A1 CA2450167 A1 CA 2450167A1
Authority
CA
Canada
Prior art keywords
ethyl
alkyl
oxa
fluoro
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002450167A
Other languages
English (en)
French (fr)
Inventor
Shon R. Pulley
James P. Beck
Ruth E. Tenbrink
Jon S. Jacobs
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Elan Pharmaceuticals LLC
Pharmacia and Upjohn Co LLC
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2450167A1 publication Critical patent/CA2450167A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
CA002450167A 2001-06-12 2002-06-12 Macrocycles useful in the treatment of alzheimer's disease Abandoned CA2450167A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US29750501P 2001-06-12 2001-06-12
US60/297,505 2001-06-12
US33308201P 2001-11-19 2001-11-19
US60/333,082 2001-11-19
PCT/US2002/018719 WO2002100399A1 (en) 2001-06-12 2002-06-12 Macrocycles useful in the treatment of alzheimer's disease

Publications (1)

Publication Number Publication Date
CA2450167A1 true CA2450167A1 (en) 2002-12-19

Family

ID=26970188

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002450167A Abandoned CA2450167A1 (en) 2001-06-12 2002-06-12 Macrocycles useful in the treatment of alzheimer's disease

Country Status (6)

Country Link
US (2) US7067507B2 (enExample)
EP (1) EP1395257A1 (enExample)
JP (1) JP2005505506A (enExample)
BR (1) BR0210391A (enExample)
CA (1) CA2450167A1 (enExample)
WO (1) WO2002100399A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008116302A1 (en) * 2007-03-26 2008-10-02 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors

Families Citing this family (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20040167A1 (es) * 2002-03-28 2004-05-26 Novartis Ag Amidas del acido sulfamico
WO2003095398A2 (en) * 2002-05-07 2003-11-20 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Polydiazeniumdiolated cyclic polyamines with polyphasic nitric oxide release and related compounds, compositions comprising same and methods of using same
AU2003232146B2 (en) * 2002-06-11 2009-06-18 Eli Lilly And Company Prodrugs of excitatory amino acids
ATE431147T1 (de) 2002-08-22 2009-05-15 Dainippon Sumitomo Pharma Co Mittel zur behandlung des integrationsdysfunktionssyndroms
DE10238722A1 (de) 2002-08-23 2004-03-11 Bayer Ag Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse
DE10238723A1 (de) * 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
DE10238724A1 (de) * 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
JP4673833B2 (ja) * 2003-01-07 2011-04-20 メルク・シャープ・エンド・ドーム・コーポレイション アルツハイマー病の治療用大環状β−セクレターゼ阻害剤
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
DE10315573A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
DE10315569A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
DE10315571A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
DE10315572A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
SE0301010D0 (sv) * 2003-04-07 2003-04-07 Astrazeneca Ab Novel compounds
SE0301009D0 (sv) * 2003-04-07 2003-04-07 Astrazeneca Ab Novel compounds
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
DE10320785A1 (de) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Arylmethyl-substituierte Pyrazolopyrimidine
US8044060B2 (en) 2003-05-09 2011-10-25 Boehringer Ingelheim International Gmbh 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory
DE10326940A1 (de) * 2003-06-16 2005-01-05 Merck Patent Gmbh Indol-Derivate
ATE457995T1 (de) 2003-06-18 2010-03-15 Tranzyme Pharma Inc Makrozyklische motilin rezeptorantagonisten
US20060142276A1 (en) * 2003-06-23 2006-06-29 Yukihiro Ohno Therapeutic agent for senile dementia
US7595316B2 (en) * 2003-06-27 2009-09-29 Banyu Pharmaceutical Co., Ltd. Heteroaryloxy nitrogenous saturated heterocyclic derivative
SA04250253B1 (ar) 2003-08-21 2009-11-10 استرازينيكا ايه بي احماض فينوكسي اسيتيك مستبدلة باعتبارها مركبات صيدلانية لعلاج الامراض التنفسية مثل الربو ومرض الانسداد الرئوي المزمن
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
DE602004012891T2 (de) 2003-12-18 2009-04-09 Janssen Pharmaceutica N.V. Pyrido- und pyrimidopyrimidinderivate als anti-proliferative mittel
DE102004001873A1 (de) * 2004-01-14 2005-09-29 Bayer Healthcare Ag Cyanopyrimidinone
HRP20040104A2 (en) * 2004-01-30 2005-10-31 Pliva-Istra�iva�ki institut d.o.o. Use of benzonaphthoazulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders
ATE437880T1 (de) * 2004-02-04 2009-08-15 Neurosearch As Dimere azacyclische verbindungen und deren verwendung
EP1713487B1 (en) * 2004-02-04 2009-12-02 Neurosearch A/S Diazabicyclic aryl derivatives as cholinergic receptor modulators
US20070160537A1 (en) * 2004-02-20 2007-07-12 Takeo Ishiyama In vivo screening method of therapeutic agent for memory/learning dysfunctions by schizophrenia
US20050239836A1 (en) 2004-03-09 2005-10-27 Varghese John Substituted hydroxyethylamine aspartyl protease inhibitors
CN1972914A (zh) * 2004-03-31 2007-05-30 詹森药业有限公司 作为组胺h3受体配合体的非咪唑杂环化合物
ATE490959T1 (de) * 2004-03-31 2010-12-15 Janssen Pharmaceutica Nv Heterocyclische nichtimidazolverbindungen als modulatoren des histamin-h3-rezeptors
GB0415320D0 (en) * 2004-07-08 2004-08-11 Astrazeneca Ab Novel compounds
WO2006010095A2 (en) 2004-07-09 2006-01-26 Elan Pharmaceuticals Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
EP1775283A4 (en) * 2004-07-14 2008-12-10 Japan Tobacco Inc 3-AMINOBENZAMIDE COMPOUND AND INHIBITORS OF THE ACTIVITY OF VANILLOID RECEPTOR 1 (VR1)
BRPI0513286A (pt) * 2004-07-15 2008-05-06 Japan Tobacco Inc compostos de benzamida condensada e inibidores de atividade de receptor vanilóide subtipo (vr1), suas composições farmacêuticas, pacote comercial, fármaco e respectivos usos
US7494986B2 (en) * 2004-07-20 2009-02-24 Bristol-Myers Squibb Company Cycloalkylamine derivatives as NK-1/SSRI antagonists
ES2306200T3 (es) * 2004-07-28 2008-11-01 Schering Corporation Inhibidores macrociclicos de beta-secretasa.
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8383637B2 (en) 2004-08-06 2013-02-26 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8426429B2 (en) 2004-08-06 2013-04-23 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
GB0418830D0 (en) 2004-08-24 2004-09-22 Astrazeneca Ab Novel compounds
CA2576782A1 (en) * 2004-08-27 2006-03-09 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using substituted ethanolcyclicamine aspartyl protease inhibitors
GB0422057D0 (en) * 2004-10-05 2004-11-03 Astrazeneca Ab Novel compounds
TW200630337A (en) * 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
CN101087609B (zh) * 2004-10-26 2012-11-14 詹森药业有限公司 因子Xa化合物
CA2587083A1 (en) * 2004-11-17 2006-05-26 Merck & Co., Inc. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
WO2006057983A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of alzheimer's disease
SI1817282T1 (sl) * 2004-11-23 2011-10-28 Astrazeneca Ab Derivati fenoksiocetne kisline, uporabni za zdravljenje respiratornih bolezni
JO3088B1 (ar) * 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
NI200700147A (es) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
DK2937341T3 (en) * 2004-12-30 2017-09-11 Janssen Pharmaceutica Nv 4- (BENZYL) -PIPERAZINE-1-CARBOXYLIC ACID PHENYLAMIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF FATTY ACID HYDROLASE (FAAH) FOR TREATING ANALYSIS, PAIN AND OTHER CONDITIONS
CA2593268A1 (en) * 2005-01-13 2006-07-20 Novartis Ag Macrocyclic compounds useful as bace inhibitors
GB0500683D0 (en) 2005-01-13 2005-02-23 Novartis Ag Organic compounds
GB0504960D0 (en) * 2005-03-10 2005-04-20 Arakis Ltd Benzoxazocines
AU2006235344B2 (en) 2005-04-08 2012-07-26 Comentis, Inc. Compounds which inhibit beta-secretase activity and methods of use thereof
EA017545B1 (ru) * 2005-06-30 2013-01-30 Янссен Фармацевтика Н.В. Циклические анилино-пиридинотриазины в качестве ингибиторов gsk-3
US7851474B2 (en) * 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
TW200745003A (en) 2005-10-06 2007-12-16 Astrazeneca Ab Novel compounds
WO2007039736A1 (en) 2005-10-06 2007-04-12 Astrazeneca Ab Novel compounds
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
ES2360957T3 (es) 2005-10-25 2011-06-10 Janssen Pharmaceutica Nv Derivados de 2-amino-3,4-dihidro-pirido(3,4-d)-pirimidina utiles como inhibidores de la beta-secretasa (bace).
JP2009514935A (ja) * 2005-11-05 2009-04-09 アストラゼネカ・アクチエボラーグ 新規化合物
WO2007068894A2 (en) * 2005-12-15 2007-06-21 Astrazeneca Ab Substituted diphenylethers, -amines, -sulfides and -methanes for the treatment of respiratory disease
US7906508B2 (en) * 2005-12-28 2011-03-15 Japan Tobacco Inc. 3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity
DE102005062986A1 (de) * 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte Propiolsäureamide und ihre Verwendung zur Herstellung von Arzneimitteln
GB0526614D0 (en) 2005-12-30 2006-02-08 Novartis Ag Organic compounds
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US7932261B2 (en) 2006-02-06 2011-04-26 Janssen Pharmaceutica Nv Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
WO2007092846A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
AU2007216531A1 (en) * 2006-02-14 2007-08-23 Neurosearch A/S Novel diazabicycloalkane derivatives and their medical use
US7795262B2 (en) * 2006-03-10 2010-09-14 Neurogen Corporation Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues
WO2007106400A2 (en) * 2006-03-10 2007-09-20 Janssen Pharmaceutica, N.V. Pyridine-containing macroheterocylic compounds as kinase inhibitors
WO2007110363A1 (en) * 2006-03-24 2007-10-04 Neurosearch A/S Novel guanidine derivatives and their medical use
WO2007110449A1 (en) * 2006-03-29 2007-10-04 Euro-Celtique S.A. Benzenesulfonamide compounds and their use
US8791264B2 (en) * 2006-04-13 2014-07-29 Purdue Pharma L.P. Benzenesulfonamide compounds and their use as blockers of calcium channels
US8937181B2 (en) * 2006-04-13 2015-01-20 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
JP2009537598A (ja) * 2006-05-23 2009-10-29 ノイロサーチ アクティーゼルスカブ 新規1,4−ジアザ−ビシクロ[3.2.2]ノナン誘導体及びそれらの医学的使用
WO2007138041A1 (en) * 2006-05-30 2007-12-06 Neurosearch A/S Novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its medical use
HRP20120852T1 (hr) * 2006-06-01 2012-11-30 Sanofi Spirocikliäśki nitrili kao inhibitori proteaze
MX2009000456A (es) * 2006-07-13 2009-01-27 Janssen Pharmaceutica Nv Derivados de quinazolina mtki.
RU2009105764A (ru) * 2006-07-20 2010-08-27 Новартис АГ (CH) Макроциклические соединения, применимые в качестве ингибиторов васе
CN101490018A (zh) * 2006-07-20 2009-07-22 诺瓦提斯公司 用作bace抑制剂的大环化合物
KR20090127307A (ko) * 2007-03-01 2009-12-10 얀센 파마슈티카 엔.브이. 히스타민 h3 수용체 조절제로서의 테트라하이드로이소퀴놀린 화합물
US8399486B2 (en) * 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
UA100983C2 (ru) * 2007-07-05 2013-02-25 Астразенека Аб Бифенилоксипропановая кислота как модулятор crth2 и интермедиаты
AU2008281849B2 (en) 2007-07-27 2013-11-28 Janssen Pharmaceutica Nv Pyrrolopyrimidines
WO2009024516A1 (en) * 2007-08-17 2009-02-26 Neurosearch A/S Novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as nicotinic acetylcholine receptor ligands
WO2009024517A1 (en) * 2007-08-17 2009-02-26 Neurosearch A/S Novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives useful as nicotinic acetylcholine receptor ligands
US8765736B2 (en) * 2007-09-28 2014-07-01 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
WO2009067401A1 (en) * 2007-11-20 2009-05-28 Janssen Pharmaceutica N.V. Cycloalkyloxy-and hetξrocycloalky- loxypyridine compounds as modulators of the histamine h3 receptor
PE20091211A1 (es) * 2007-11-30 2009-09-14 Boehringer Ingelheim Int Derivados de pirazolopirimidina como moduladores de pde9a
WO2009097278A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
MX2010008243A (es) 2008-01-29 2010-11-30 Janssen Pharmaceutica Nv Derivados de 2-aminoquinolina utiles como inhibidores de beta-secretasa (bace).
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
US8236792B2 (en) * 2008-05-23 2012-08-07 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine H3 receptor
EA201100446A1 (ru) 2008-09-08 2011-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Пиразолопиримидины и их применение для лечения нарушений цнс
AU2010230290B2 (en) * 2009-03-31 2013-03-14 Boehringer Ingelheim International Gmbh 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as PDE9A modulators
JP5768239B2 (ja) * 2009-05-07 2015-08-26 株式会社 PRISM BioLab アルファへリックスミメティック及び関連の方法
CA2764124C (en) * 2009-06-19 2016-12-13 D. Western Therapeutics Institute, Inc. Substituted isoquinoline derivative
JP2012530084A (ja) * 2009-06-19 2012-11-29 アボット・ラボラトリーズ ジアザホモアダマンタン誘導体およびこの使用方法
AR077859A1 (es) * 2009-08-12 2011-09-28 Boehringer Ingelheim Int Compuestos para el tratamiento de trastornos del snc
DK2603511T3 (en) 2010-08-12 2017-05-08 Boehringer Ingelheim Int 6-CYCLOALKYL-1, 5-DIHYDRO-PYRAZOLO- [3,4-D] PYRIMIDIN-4-ON DERIVATIVES AND THEIR USES AS PDE9A INHIBITORS
ES2380473B1 (es) * 2010-10-13 2013-02-19 Neuron Biopharma, S.A. Compuesto neuroprotector, hipocolesterolémico, antiinflamatorio y antiepiléptico.
US8258139B2 (en) 2010-11-08 2012-09-04 Dainippon Sumitomo Pharma Co., Ltd. Method of treatment for mental disorders
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
KR102010222B1 (ko) 2011-04-05 2019-08-13 슬로안-케테링인스티튜트퍼캔서리서치 Hsp90 억제제
CN103596955B (zh) * 2011-04-05 2016-11-16 索隆-基特林癌症研究协会 Hsp90抑制剂
DK2721012T3 (en) 2011-06-17 2016-08-15 Lilly Co Eli Biclo (3.1.0) hexane-2,6-dicarboxylic acid derivatives as MGLU2 receptor agonist
IN2014KN01075A (enExample) 2011-11-18 2015-10-09 Heptares Therapeutics Ltd
US20150141500A1 (en) * 2012-05-10 2015-05-21 Mahesh Kandula Compositions and methods for the treatment of neurological diseases
US20150141384A1 (en) * 2012-07-03 2015-05-21 Mahesh Kandula Compositions and methods for the treatment of neurological degenerative disorders
FR2993563B1 (fr) * 2012-07-20 2015-12-18 Metabrain Res Derives de thiophenes utiles dans le traitement du diabete
PT2909204T (pt) 2012-10-12 2019-03-21 Dana Farber Cancer Inst Inc Inibidores de gsk3 e métodos de utilização dos mesmos
CA2887598A1 (en) 2012-10-12 2014-04-17 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
WO2014075676A1 (en) * 2012-11-15 2014-05-22 V-Biotek Holding Aps Amines from trigonella foemum - graecum
AU2014249192B2 (en) * 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
UA117695C2 (uk) * 2014-02-19 2018-09-10 Х. Луннбек А/С 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера
GB201404922D0 (en) 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
MX375990B (es) * 2014-04-11 2025-03-07 Takeda Pharmaceuticals Co Compuesto de ciclopropanamina y sus usos.
WO2015170683A1 (ja) * 2014-05-09 2015-11-12 サントリーホールディングス株式会社 メトキシフラボンを含むNOX阻害剤及びNFκB阻害剤
WO2015195950A1 (en) * 2014-06-20 2015-12-23 Principia Biophamram Inc. Lmp7 inhibitors
TW201625639A (zh) * 2014-09-17 2016-07-16 腫瘤設計公司 巨環lrrk2激酶抑制劑
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
AU2016226463B2 (en) * 2015-03-03 2020-06-25 Biohaven Pharmaceutical Holding Company Ltd. Riluzole prodrugs and their use
WO2016149248A1 (en) * 2015-03-15 2016-09-22 Emory University N-methyl-d-aspartate receptor (nmdar) potentiators, pharmaceutical compositions, and uses related thereto
AR105025A1 (es) * 2015-06-19 2017-08-30 Astellas Pharma Inc Compuesto de imidazodiazepina
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
TN2018000035A1 (en) 2015-08-12 2019-07-08 H Lundbeck As 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
GB201519352D0 (en) * 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
EP4302764A3 (en) * 2016-07-11 2024-06-26 Sage Therapeutics, Inc. C17, c20, and c21 substituted neuroactive steroids and their methods of use
EP3493803A4 (en) * 2016-08-05 2020-04-22 The Regents of The University of California GP130 MODULATORS
SMT202200331T1 (it) * 2016-10-05 2022-09-14 Nsc Therapeutics Gmbh Polimorfi cristallini di un agonista di recettore muscarinico di acetilcolina
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
US20190388425A1 (en) * 2017-01-20 2019-12-26 Bayer Pharma Aktiengesellschaft Substituted imidazopyridinpyrimidines
EP3596078B1 (en) * 2017-03-15 2023-04-12 UCB Biopharma SRL Fused pentacyclic imidazole derivatives as modulators of tnf activity
JP7157075B2 (ja) * 2017-04-05 2022-10-19 ザ ブロード インスティテュート,インコーポレーテッド グリコーゲンシンターゼキナーゼ3(gsk3)インヒビターとしての三環式化合物およびそれらの使用
EP3625232B1 (en) * 2017-05-19 2021-06-23 Council of Scientific and Industrial Research Substituted methanopyrido [2, 1-a]isoindolones as machr modulators for treating various associated pathophysiological conditions and process for preparation thereof
GB201712567D0 (en) * 2017-08-04 2017-09-20 Karin & Sten Mortstedt Cbd Solutions Ab Selective ligands for tau aggregates
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
EP4076659A1 (en) * 2019-12-19 2022-10-26 Latvian Institute Of Organic Synthesis Macrocyclic amides acting as plasmepsin inhbitors for the treatment of malaria

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPM982594A0 (en) 1994-12-02 1995-01-05 University Of Queensland, The HIV protease inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008116302A1 (en) * 2007-03-26 2008-10-02 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors

Also Published As

Publication number Publication date
WO2002100399A1 (en) 2002-12-19
US7456163B2 (en) 2008-11-25
US7067507B2 (en) 2006-06-27
BR0210391A (pt) 2004-06-15
JP2005505506A (ja) 2005-02-24
US20030236240A1 (en) 2003-12-25
EP1395257A1 (en) 2004-03-10
US20060003978A1 (en) 2006-01-05

Similar Documents

Publication Publication Date Title
CA2450167A1 (en) Macrocycles useful in the treatment of alzheimer's disease
EP1409450B1 (en) N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds
US7312360B2 (en) Substituted hydroxyethylamines
US6962934B2 (en) Substituted amino carboxamides for the treatment of Alzheimer's disease
US6982264B2 (en) Substituted alcohols useful in treatment of Alzheimer's disease
US20060100196A1 (en) Substituted amines for the treatment of alzheimer's disease
CA2453447A1 (en) Alpha-hydroxyamide statine derivatives for the treatment of alzheimer's disease
EP1404671B1 (en) Macrocycles useful in the treatment of alzheimer's disease
CA2462851A1 (en) Hydroxypropylamines
US20030092747A1 (en) Aminediols for the treatment of Alzheimer's disease
US20040039034A1 (en) Hydroxypropyl amides for the treatment of Alzheimer's disease
US20030096864A1 (en) Compounds to treat alzheimer's disease
US7566730B2 (en) Substituted aminoethers for the treatment of Alzheimer's disease
WO2004029019A2 (en) Compounds for the treatment of alzheimer’s disease
MXPA03011442A (es) Macrociclos utiles en tratamiento de enfermedad de alzheimer.
WO2005042472A2 (en) Hydroxypropyl amides for the treatment of alzheimer’s disease

Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued
FZDE Discontinued

Effective date: 20100614