AR049654A1 - Derivados de tetrahidroquinolina como reguladores de proteinas motoras mitoticas - Google Patents

Derivados de tetrahidroquinolina como reguladores de proteinas motoras mitoticas

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Publication number
AR049654A1
AR049654A1 ARP050102681A ARP050102681A AR049654A1 AR 049654 A1 AR049654 A1 AR 049654A1 AR P050102681 A ARP050102681 A AR P050102681A AR P050102681 A ARP050102681 A AR P050102681A AR 049654 A1 AR049654 A1 AR 049654A1
Authority
AR
Argentina
Prior art keywords
nnr2
naryl
nheteroaryl
nxr
xch
Prior art date
Application number
ARP050102681A
Other languages
English (en)
Inventor
Kai Schiemann
David Bruge
Hans-Peter Buchstaller
Dirk Finsinger
Wolfgang Staehle
Christiane Amendt
Ulrich Emde
Frank Zenke
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 AR049654A1 publication Critical patent/AR049654A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de la formula (1), en la que: W es CH o N; R1, R2, R3 son, de modo independiente entre sí, H, A, arilo, heteroarilo, Hal, -(CY2)n-SA, -(CY2)n-SCF3, -(CY2)n-SCN, -(CY2)n-CF3, -(CY2)n-OCF3, cicloalquilo, -SCH3, -SCN, -CF3, -OCF3, -OA, - (CY2)n-OH, -(CY2)n-CO2R, -(CY2)n-CN, -(CY2)n-Hal, -(CY2)n-NR2, (CY2)n-OA, (CY2)n-OCOA, -SCF3, (CY2)n-CONR2, -(CY2)n-NHCOA, -(CY2)n-NHSO2A; Y es H, A Hal; A es alquilo o cicloalquilo; Hal es F, Cl, Br o I; R es H o A, en caso de radicales geminales R también son juntos -(CH2)5-, -(CH2)4- o -(CH2)2-NR-(CH2)2; R4, R5 son juntos -X(CH2)2X-, -X(CR2)X-, -XCH(CH2OR)X-, -XCH(CH2OR)CR2X-, -XCR2CH(CH2OR)X-, -XCH(CH2NR2)X-, -XCH(CH2NR2)CR2X-, -XCR2CH(CH2NR2)X-, -OCH2CH2O-, -X(CH2)2X-, -XCHQCR2X, -XCR2CHQX- , -XCR2X-, -XCH(CH2OR)X-, -XCH(CH2OR)CR2X-, -X-C(=X)-X-, -XCH(CH2NR2)X-, -XCH(CH2NR2)CR2X-, -OCH2CH2O-, -X-C(=X)-X-; Q es CH2Hal, CHO, CORa, CH2Ra, CH2OCORa, CH2NCOR1, CH2N(R1)2, CH2OR1, CH2OCON(R1)2, CH2OCOOR1, CH2NHCON(R1)2, CH2NHCOOR1; Ra es un resto seleccionado del grupo de formulas (2), OR, NHR2, NR2OR, NHR2, NR2, NR(CH2)narilo, NR(CH2)nOR, COOR, radical de N-pirrolidona, OCOR, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNHCOOR]COarilo, R1, N[CH2(CH2)nOR]2, NR(CH2)nNCOOR, X(CH2)nX(CH2)nXR, NR(CH2)nX(CH2)nOH, NR(CH2)nO(CH2)nOH, (CH2)nCOOR, O(CO)NR(CH2)OR, O(CO)(CH2)nNR2, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nR1, N(R)(CH2)nN(R)COOR, XCOO(CH2)nNR2, OSO2A, OSO2CF3, OSO2Ar, OCONR2, OCH2(CH2)nNR2; Z es CH2, X, CHCONH2, CH(CH2)nNRCOOR, CHNRCOOR, NCO, CH(CH2)nCOOR, NCOOR, CH(CH2)nOH, N(CH2)nOH, CHNH2, CH(CH2)nNR2, CH(CH2)nNR2, C(OH)R, CHNCOR, CH(CH2)narilo, CH(CH2)nheteroarilo, CH(CH2)nR1, N(CH2)nCOOR, CH(CH2)nX(CH2)narilo, CH(CH2)nX(CH2)nheteroarilo, N(CH2)nCONR2, XCONR(CH2)nNR2, N[(CH2)nXCOOR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nXarilo, N[(CH2)nXR]SO2(CH2)narilo, N[(CH2)nNRCOOR]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)nNRarilo, N[(CH2)nNR2]SO2(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nXR]CO(CH2)nXheteroarilo, N[(CH2)nXR]SO2(CH2)nheteroarilo, N[(CH2)nNRCOOR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nNRheteroarilo, N[(CH2)nNR2]SO2(CH2)nheteroarilo, O(CH2)nNR2, X(CH2)nNR2, NCO(CH2)nNR2, X es O, S o NR; R6 es arilo o heteroarilo insustituido o mono- o polisustituido con arilo o heteroarilo, que puede estar sustituido con Hal, NO2, CN, A, OR, OCOR, NR2, CF3, OCF3, OCH(CF3)2, Hal, NO2, CN, OR, A, -(CY2)n-OR, -OCOR, -(CY2)n-CO2R, -(CY2)n-CN o -(CY2)n-NR2; R7 es (C=O)-R, (C=O)-NR2, (C=O)-OR, H o A; y n, m son, de modo independiente entre sí, 0, 1, 2, 3, 4, 5, 6 o 7, así como sus derivados, solvatos, tautomeros, sales y estereoisomeros de utilidad farmacéutica, así como sus mezclas en todas las proporciones, pueden ser utilizados, por ejemplo, para el tratamiento de tumores.
ARP050102681A 2004-06-30 2005-06-29 Derivados de tetrahidroquinolina como reguladores de proteinas motoras mitoticas AR049654A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004031656A DE102004031656A1 (de) 2004-06-30 2004-06-30 Tetrahydrochinoline

Publications (1)

Publication Number Publication Date
AR049654A1 true AR049654A1 (es) 2006-08-23

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ID=35063029

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ARP050102681A AR049654A1 (es) 2004-06-30 2005-06-29 Derivados de tetrahidroquinolina como reguladores de proteinas motoras mitoticas

Country Status (14)

Country Link
US (1) US7915416B2 (es)
EP (1) EP1778694A1 (es)
JP (1) JP5121450B2 (es)
KR (1) KR20070037585A (es)
CN (1) CN1976936A (es)
AR (1) AR049654A1 (es)
AU (1) AU2005259676B2 (es)
BR (1) BRPI0512784A (es)
CA (1) CA2572350C (es)
DE (1) DE102004031656A1 (es)
MX (1) MXPA06014293A (es)
RU (1) RU2007103300A (es)
WO (1) WO2006002726A1 (es)
ZA (1) ZA200700819B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007013854A1 (de) * 2007-03-20 2008-09-25 Merck Patent Gmbh Tetrahydrochinoline
AU2008312401C1 (en) 2007-10-19 2014-07-10 Merck Sharp & Dohme Llc Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting KSP kinesin activity
EP2647638A1 (en) * 2012-04-02 2013-10-09 Almirall, S.A. Substituted tricyclic compounds with activity towards ep1 receptors
CN109666666B (zh) * 2019-01-21 2021-03-05 天津科技大学 一种基于分子动力学的酶柔性分析提高肝素酶i热稳定性的突变体及其制备方法
CN111233761B (zh) * 2020-03-16 2022-01-14 大连理工大学 一类2-取代四氢喹啉化合物及其衍生物、制备方法和应用
WO2022006365A2 (en) * 2020-07-02 2022-01-06 Purdue Research Foundation Tetrahydro-3h-pyrazolo quinolone and tetrahydro-3h-pyrrolo[3,2-f]quinoline-containing compounds and uses thereof

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Also Published As

Publication number Publication date
AU2005259676A1 (en) 2006-01-12
DE102004031656A1 (de) 2006-01-19
CN1976936A (zh) 2007-06-06
ZA200700819B (en) 2008-01-30
WO2006002726A1 (de) 2006-01-12
CA2572350A1 (en) 2006-01-12
JP2008505136A (ja) 2008-02-21
KR20070037585A (ko) 2007-04-05
US7915416B2 (en) 2011-03-29
RU2007103300A (ru) 2008-08-10
AU2005259676B2 (en) 2011-03-10
MXPA06014293A (es) 2007-02-19
CA2572350C (en) 2013-02-19
JP5121450B2 (ja) 2013-01-16
BRPI0512784A (pt) 2008-04-08
EP1778694A1 (de) 2007-05-02
US20090030028A1 (en) 2009-01-29

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