PE20051006A1 - Compuestos de lactamas macrociclicas como inhibidores de proteasas asparticas - Google Patents

Compuestos de lactamas macrociclicas como inhibidores de proteasas asparticas

Info

Publication number
PE20051006A1
PE20051006A1 PE2004001073A PE2004001073A PE20051006A1 PE 20051006 A1 PE20051006 A1 PE 20051006A1 PE 2004001073 A PE2004001073 A PE 2004001073A PE 2004001073 A PE2004001073 A PE 2004001073A PE 20051006 A1 PE20051006 A1 PE 20051006A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
cycloalkyl
ethyl
aspartic proteases
Prior art date
Application number
PE2004001073A
Other languages
English (en)
Inventor
Yves Auberson
Claudia Betschart
Kurt Laumen
Rainer Machauer
Marina Tintelnot-Blomley
Thomas J Troxler
Siem Jacob Veenstra
Ralf Glatthar
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20051006A1 publication Critical patent/PE20051006A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • 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
    • 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
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/02—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES CH(RE)C(=O)N(RA)RB, (CH2)KN(RC)RD; K ES 0-2; RA Y RB SON CADA UNO H, ALQUILO C1-C8 SUSTITUIDO O NO, CICLOALQUILO C3-C7, ARILO, ENTRE OTROS; RC Y RD SON CADA UNO H, ALQUILO C1-C8 SUSTITUIDO O NO, CICLOALQUILO C3-C7, HETEROARILO, ENTRE OTROS; RE ES ALQUILO C1-C8, CICLOALQUILO C3-C7, ENTRE OTROS; R2 ES H, ALQUILO C1-C4; R3 ES H, ALQUILO C1-C6, ARILALQUILO C1-C4(OC(=O)NH), ENTRE OTROS; U ES UN ENLACE, CF2, CHF, CICLOPROP-1,2-ILENO, ENTRE OTROS; V ES CH=CH, CH2CH(OH), CH(OH)CH2, ENTRE OTROS; W ES ALQUILENO C1-C6, O, S S(=O)2, ENTRE OTROS; X ES ALCANILILIDENO C1-C4 SUSTITUIDO O NO, ALQUILENO C1-C4, PIPERIDIN-DIILO, ENTRE OTROS; Y ES ENLACE, O, S(=O)2, NHS(=O)2, NH, ENTRE OTROS; Z ES O, CH2, CF2, CHF, ENTRE OTROS; n ES 0-5. SON COMPUESTOS PREFERIDOS: (3S,14R)-16-[1-HIDROXI-2-(3-METIL-BENCILAMINO)-ETIL]-3,4,14-TRIMETIL-1,4-DIAZA-CICLOHEXADECANO-2,5-DIONA; (4S,6R)-12-ETIL-4-[(1R)-1-HIDROXI-2-(3-ISOPROPIL-BENCILAMINO)-ETIL]-6-METIL-3,12-DIAZA-BICICLO[12.3.1]OCTADECA-1(17),14(18),15-TRIEN-2,13-DIONA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE PROTEASAS ASPARTICAS, PATICULARMENTE BETA-SECRETASA UTILES EN ELTRATAMIENTO DE DE TRASTORNOS NEUROLOGICOS O VASCULARES
PE2004001073A 2003-11-05 2004-11-04 Compuestos de lactamas macrociclicas como inhibidores de proteasas asparticas PE20051006A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0325830.8A GB0325830D0 (en) 2003-11-05 2003-11-05 Organic compounds

Publications (1)

Publication Number Publication Date
PE20051006A1 true PE20051006A1 (es) 2005-12-28

Family

ID=29725994

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004001073A PE20051006A1 (es) 2003-11-05 2004-11-04 Compuestos de lactamas macrociclicas como inhibidores de proteasas asparticas

Country Status (15)

Country Link
US (2) US7612055B2 (es)
EP (1) EP1682521A1 (es)
JP (1) JP4628366B2 (es)
KR (1) KR20060110289A (es)
CN (1) CN1902182A (es)
AR (1) AR046321A1 (es)
AU (1) AU2004291276B2 (es)
BR (1) BRPI0416276A (es)
CA (1) CA2544751A1 (es)
GB (1) GB0325830D0 (es)
MX (1) MXPA06005032A (es)
PE (1) PE20051006A1 (es)
RU (1) RU2006119504A (es)
TW (1) TW200530203A (es)
WO (1) WO2005049585A1 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0312439A (pt) * 2002-06-20 2005-05-10 Pharmacia & Upjohn Co Llc Processo para preparação de derivados de ácido 5-(1,3-oxazol-2-il)benzóico
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
US8426429B2 (en) 2004-08-06 2013-04-23 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
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)
MX2007008507A (es) * 2005-01-13 2009-02-16 Novartis Ag Compuestos macrociclicos utiles como inhibidores de bace.
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
WO2007021793A1 (en) 2005-08-12 2007-02-22 Bristol-Myers Squibb Company Macrocyclic diaminopropanes as beta-secretase inhibitors
CN104744234A (zh) * 2005-08-19 2015-07-01 爱密斯菲尔科技公司 用于递送活性剂的环丙基化合物和组合物
PL1966198T3 (pl) 2005-10-25 2011-07-29 Janssen Pharmaceutica Nv Pochodne 2-amino-3,4-dihydropirydo[3,4-d]pirymidyny do zastosowania jako inhibitory beta-sekretazy (BACE)
GB0526614D0 (en) * 2005-12-30 2006-02-08 Novartis Ag Organic compounds
WO2007092839A2 (en) * 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
US7868022B2 (en) 2006-02-06 2011-01-11 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
WO2008009734A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams
BRPI0715440A2 (pt) * 2006-07-20 2013-07-23 Novartis Ag compostos macrocÍclicos éteis como inibidores de bace
US7678784B2 (en) 2006-11-20 2010-03-16 Bristol-Myers Squibb Company Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors
US7772221B2 (en) 2007-02-09 2010-08-10 Bristol-Meyers Squibb Company Diaminopropane derived macrocycles as inhibitors of β amyloid production
JP5526018B2 (ja) * 2007-03-21 2014-06-18 エミスフェアー・テクノロジーズ・インク アリルオキシおよびアルキルオキシ安息香酸送達薬剤
US7732434B2 (en) 2007-04-20 2010-06-08 Bristol-Myers Squibb Company Macrocyclic acyl guanidines as beta-secretase inhibitors
WO2008135488A1 (en) * 2007-05-04 2008-11-13 Medivir Ab Aspartyl protease inhibitors
JP2011510989A (ja) 2008-01-28 2011-04-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ β−セクレターゼ（ＢＡＣＥ）の阻害物質として有用な６−置換−チオ−２−アミノ−キノリン誘導体
CA2714008A1 (en) 2008-01-29 2009-08-06 Janssen Pharmaceutica N.V. 2-amino quinoline derivatives useful as inhibitors of .beta.-secretase (bace)
WO2010058577A1 (ja) * 2008-11-20 2010-05-27 株式会社カネカ 不飽和アミノカルボン酸誘導体の製造方法
ES2649964T3 (es) 2011-02-08 2018-01-16 Merck Patent Gmbh Derivados de aminoestatina para el tratamiento de la artrosis
ES2564972T3 (es) 2011-03-18 2016-03-30 Bayer Intellectual Property Gmbh Derivados de N-(3-carbamoilfenil)-1H-pirazol-5-carboxamida y su uso para combatir parásitos animales
US9624264B2 (en) 2012-07-24 2017-04-18 Merck Patent Gmbh Hydroxystatin derivatives for the treatment of arthrosis
ES2612982T3 (es) 2013-02-25 2017-05-19 Merck Patent Gmbh Derivados de 2-amino-3,4-dihidroquinazolina y su aplicación como inhibidores de la catepsina D
CN105451754A (zh) 2013-08-06 2016-03-30 默克专利股份有限公司 在关节病的情况下胃酶抑素的关节内施用
WO2019075259A1 (en) * 2017-10-11 2019-04-18 Cornell University MACROCYCLIC COMPOUNDS AS PROTEASE INHIBITORS
JP7444170B2 (ja) * 2019-09-02 2024-03-06 株式会社レゾナック イオン性化合物、有機エレクトロニクス材料、有機層、有機エレクトロニクス素子、有機エレクトロルミネセンス素子、表示素子、照明装置、及び有機エレクトロニクス素子の製造方法
CN116199702A (zh) * 2021-12-01 2023-06-02 上海交通大学医学院附属仁济医院 一种大环内酰胺类化合物、其制备方法及应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05508167A (ja) 1991-04-17 1993-11-18 エフ・ホフマン―ラ　ロシュ　アーゲー 新規なｄｎａジャイレース阻害剤、その製造方法およびそれらを含有する製薬学的製剤
TW343965B (en) 1994-03-30 1998-11-01 Hoffmann La Roche Novel mono- and bicyclic DNA gyrase inhibitors
BR0210391A (pt) * 2001-06-12 2004-06-15 Elan Pharm Inc Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto
ATE323084T1 (de) * 2001-06-12 2006-04-15 Elan Pharm Inc Für die behandlung von alzheimer krankheit geeignete makrocyclen
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
MX2007008507A (es) * 2005-01-13 2009-02-16 Novartis Ag Compuestos macrociclicos utiles como inhibidores de bace.
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
GB0526614D0 (en) * 2005-12-30 2006-02-08 Novartis Ag Organic compounds
WO2008009734A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams
BRPI0715440A2 (pt) * 2006-07-20 2013-07-23 Novartis Ag compostos macrocÍclicos éteis como inibidores de bace

Also Published As

Publication number Publication date
MXPA06005032A (es) 2006-07-06
AU2004291276B2 (en) 2009-03-12
JP4628366B2 (ja) 2011-02-09
WO2005049585A1 (en) 2005-06-02
BRPI0416276A (pt) 2007-01-23
US7612055B2 (en) 2009-11-03
GB0325830D0 (en) 2003-12-10
RU2006119504A (ru) 2007-12-27
AU2004291276A1 (en) 2005-06-02
AR046321A1 (es) 2005-11-30
CN1902182A (zh) 2007-01-24
CA2544751A1 (en) 2005-06-02
JP2007510002A (ja) 2007-04-19
KR20060110289A (ko) 2006-10-24
EP1682521A1 (en) 2006-07-26
US20070072792A1 (en) 2007-03-29
TW200530203A (en) 2005-09-16
US20100022500A1 (en) 2010-01-28

Similar Documents

Publication Publication Date Title
PE20051006A1 (es) Compuestos de lactamas macrociclicas como inhibidores de proteasas asparticas
PE20070218A1 (es) COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA
PE20070138A1 (es) Compuestos heterociclicos como inhibidores de aspartil proteasas
PE20070115A1 (es) Derivados de [1,3,5]-triazina como inhibidores de aspartil proteasas
MA27582A1 (fr) Derives benzazepine pour le traitement de troubles neurologiques
CA2135474A1 (en) Thiazolidine Derivatives and Pharmaceutical Compositions Containing the Same
CA2383298A1 (fr) Nouveaux derives d'.alpha.-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2545427A1 (en) Selective kinase inhibitors
MXPA04000293A (es) Inhibidores de serina proteasa biciclica de puente.
AR039203A1 (es) Derivados de quinazolina
WO2004087699A3 (en) Thiazoles useful as inhibitors of protein kinases
WO2004087698A3 (en) Thiazoles useful as inhibitors of protein kinases
PE20040974A1 (es) Compuestos de amida de acido carboxilico con efecto antagonico de la hcm, medicamentos que los contienen y procedimientos para su preparacion
GEP20094723B (en) Tetraazabenzo [e] azulene derivatives and analogs thereof
NO20056192L (no) Kapaseinhibitorer og anvendelse derav
WO2005063745A3 (en) Novel spiroindoline or spiroisoquinoline compounds, methods of use and compositions thereof
IL169316A (en) Small molecules modulate hepatocyte growth factor (dispersion factor)
BG100692A (en) New heterocyclic compounds
EP1396493A4 (en) HETEROCYCLIC COMPOUNDS
ATE476431T1 (de) Piperidin- und azetidinderivate als glyt1- inhibitoren
ZA200408283B (en) 7-aryl-3,9-diazabicyclo (3.3.1)non-6-ene derivatives and their use as renin inhibitors in the treatment of hypertension, cardivascular or rental diseases
AU2003250471A8 (en) Pyrimidine-2,4-dione derivatives as matrix metalloproteinase inhibitors
TR200102524T2 (tr) Dihetero sübstitüe edilmiş metaloproteaz inhibitörleri.
WO2006036981A3 (en) Small molecule modulators of cytokine activity
WO2004014389A8 (en) 3,4-dihydroquinolin-2-one, 5,6-fused oxazin-3-one, and 5,6-fused thiazin-3-one derivatives as matrix metalloproteinase inhibitors

Legal Events

Date Code Title Description
FC Refusal