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AR072098A1 - Derivados de pirrolidina como inhibidores de metap-2 - Google Patents

Derivados de pirrolidina como inhibidores de metap-2

Info

Publication number
AR072098A1
AR072098A1 ARP090102101A ARP090102101A AR072098A1 AR 072098 A1 AR072098 A1 AR 072098A1 AR P090102101 A ARP090102101 A AR P090102101A AR P090102101 A ARP090102101 A AR P090102101A AR 072098 A1 AR072098 A1 AR 072098A1
Authority
AR
Argentina
Prior art keywords
mar1
mhet2
hal
nhcoch
coch
Prior art date
Application number
ARP090102101A
Other languages
English (en)
Inventor
Frank Zenke
Holger Enderle
Timo Heinrich
Alfred Jonczyk
Mireille Krier
Thorsten Knoechel
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR072098A1 publication Critical patent/AR072098A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Los compuestos de la formula (1) en donde Z es un resto del grupo de formulas (2); R1, R2 son cada uno, de modo independiente entre s¡, H, A, Hal, NH2, (CH2)mHet2, (CH2)mCOOR6 o (CH2)mCONH2; X1 es CH o N; X2 es CH o N; R3, R4 son cada uno, de modo independiente entre s¡, H, Hal, OH o NH2; R6 es H o alquilo C1-6; X es O, NH, NA, OC(=O) o est  ausente; Y es CH=CH o (CH2)n; R es Ar, Het o Carb1; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, OR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2N(R6)2, S(O)qA, SO2OH, CH=CH-CONH(CH2)pOH, NHCONH-Het, NHCONHA, (CH2)mAr1, O(CH2)mAr1, O(CH2)mHet2, O(CH2)mCOOR6, un resto de formula (3), (CH2)mHet, CH2NH[(CH2)2O]q[(CH2)2O]q(CH2)pNH2, CH2N(COA)CH2CH(OH)CH2OH, CH2NH(CH2)qHet, CH2N(COA) (CH2)qHet, CH2N(CHO)(CH2)qHet, COHet, NHCOCH[(CH2)mCOOA]NHCOO(CH2)mAr1, NHCOCH[(CH2)mCONH2]NHCOOA, NHCOCH[(CH2)mCOOH]NHCOOH, NHCOCH[(CH2)mHet2]NHCOOA, NHCOCH[(CH2)mHet2]NH2, NHCOCH[(CH2)mCONH2]NH2, CH=CH-COOR6 y/o CH=CH-CON(R6)2; Het es un heterociclo saturado, insaturado o arom tico mono-, di- o tric¡clico no sustituido o mono-, di- o trisustituido con Hal, A, (CH2)mOR6, N(R6)2, NO2, (CH2)mCN, (CH2)mCOOR6, CONH(CH2)mCOOH, CONH(CH2)mHet2, CO(CH2)mN(R6)2, CO(CH2)mNH(CH2)rCOOA, COO(CH2)mAr1, (CH2)rCONH(CH2)mAr1, COCH[(CH2)mCONH2]NH2, COCH[(CH2)mCONH2]NHCOOA, COCH[(CH2)mHet2)NHCOOA, COCH[(CH2)mHet2]NH2, COCH[(CH2)mNHCOOA]NHCOO(CH2)mAr1, COCH[(CH2)mNH2]NHCOO(CH2)mAr1, NR6COA, NR6SO2A, COR6, SO2NR6, S(O)qA, NHCONH-(CH2)m-Cyc-OR6, CONH(CH2)pOR6, O(CH2)pOR6, CHO, (CH2)mHet2, COHet2, (CH2)rNH(CH2)mHet2, (CH2)mNH(CH2)mAr1, NH(CH2)pN(R6)2, (CH2)mAr1, O(CH2)mAr1 y/u =O (ox¡geno del carbonilo) con 1 a 4  tomos de N y/u O y/o S, y en donde un N tambien puede estar oxidado; Cyc es cicloalquileno C3-7; Ar1 es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, OR6, COOR6, CON(R6)2, NR6COA y/o CONH(CH2)pHet2; Carb1 es un resto seleccionado del grupo de formulas (4); R5 es OR6, COOR6, CON(R6)2 o Het1; R7 es (CH2)rCON(R6)2, (CH2)rCON[(CH2CH2)OH]2 o (CH2)rCONH(CH2CH2)OH; Het1 es imidazolilo, pirazolilo o 4-cloro-2-metil-pirazolilo; Het2 es un heterociclo arom tico o saturado monoc¡clico no sustituido o mono-, di- o trisustituido con Hal, A, OR6, NHCOA, N(R6)2 y/u =O (ox¡geno del carbonilo) con 1 a 2  tomos de N y/u O y/o S; A es alquilo no ramificado o ramificado C1-10, en donde 1-7  tomos de H pueden estar reemplazados por F, Cl, Br y/u OH, o alquilo c¡clico con 3-7  tomos de C; Hal es F, Cl, Br o I; m es 0, 1, 2, 3, 4, 5 o 6; n es 1 o 2; p es 1, 2, 3 o 4; q es 0, 1, 2, 3 o 4; r es 0, 1 o 2; as¡ como sus sales, tautomeros y estereoisomeros farmaceuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la metionina-amino-peptidasa y se pueden usar para el tratamiento de tumores.
ARP090102101A 2008-06-10 2009-06-10 Derivados de pirrolidina como inhibidores de metap-2 AR072098A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008027574A DE102008027574A1 (de) 2008-06-10 2008-06-10 Neue Pyrrolidinderivate als MetAP-2 Inhibitoren

Publications (1)

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AR072098A1 true AR072098A1 (es) 2010-08-04

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US (1) US8846694B2 (es)
EP (1) EP2288351B1 (es)
JP (1) JP5654456B2 (es)
AR (1) AR072098A1 (es)
AU (1) AU2009267539B2 (es)
CA (1) CA2727282C (es)
DE (1) DE102008027574A1 (es)
ES (1) ES2694754T3 (es)
IL (1) IL209477A (es)
WO (1) WO2010003475A2 (es)

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EP2288351B1 (de) 2018-08-08
ES2694754T3 (es) 2018-12-27
JP2011527295A (ja) 2011-10-27
WO2010003475A8 (de) 2011-01-20
US8846694B2 (en) 2014-09-30
CA2727282C (en) 2016-08-23
CA2727282A1 (en) 2010-01-14
WO2010003475A3 (de) 2010-04-29
IL209477A (en) 2017-07-31
JP5654456B2 (ja) 2015-01-14
DE102008027574A1 (de) 2009-12-17
US20110263561A1 (en) 2011-10-27
AU2009267539B2 (en) 2013-09-12
EP2288351A2 (de) 2011-03-02
IL209477A0 (en) 2011-01-31

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