AR054615A1 - Tetrahidroquinolinas - Google Patents

Tetrahidroquinolinas

Info

Publication number
AR054615A1
AR054615A1 ARP060102410A ARP060102410A AR054615A1 AR 054615 A1 AR054615 A1 AR 054615A1 AR P060102410 A ARP060102410 A AR P060102410A AR P060102410 A ARP060102410 A AR P060102410A AR 054615 A1 AR054615 A1 AR 054615A1
Authority
AR
Argentina
Prior art keywords
nnr2
naryl
nheteroaryl
nxr
aryl
Prior art date
Application number
ARP060102410A
Other languages
English (en)
Inventor
Kai Schiemann
David Bruge
Hans-Peter Buchstaller
Ulrich Emde
Dirk Finsinger
Christiane Amendt
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 AR054615A1 publication Critical patent/AR054615A1/es

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Classifications

    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuestos de formula (1), donde: W es CH o N; R 1, R2, R3 independientemente 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-Hal, -(CH2)nR, -(CY2)n-NR2, -(CY2)n-OR, -(CY2)n-OCOA, -SCF3, -(CY2)n-CONR2, -(CY2)n-NHCOA, -(CY2)n-NHSO2A, SF5, Si(CH3)3, CO-(CY2)n-CH3, -(CY2)n-N-pirrolidona, -(CH2)nNRCOOR, NRCOOR, NCO, CH2(CH2)nCOOR, NHCOOR, CH2-(CH2)n-OH, - NR(CH2)nOH, CH2NH2, (CH2)nNR2, CH(OH)R2, CH2NHCOR, (CH2)narilo, CH2(CH2)nheteroarilo, (CH2)nR1, NH(CH2)nCOOR, CH2(CH2)nX(CH2)narilo, (CH2)(CH2)nX(CH2)nheteroarilo, NH(CH2)nCONR2, XCONR(CH2)nNR2, N[(CH2)nXCOOR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nX-arilo, N[(CH2)nXR]SO2(CH2)narilo, N[(CH2)nNRCOOR]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)nNR-arilo, N[(CH2)nNR2]SO2(CH2)narilo, N[(CH2)nXR]CO(CH2)nheteroarilo, N[(CH2)nXR]CO(CH2)nX-heteroarilo, N[(CH2)nXR]SO2(CH2)nheteroarilo, N[(CH2)nNRCOOR]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nNR-heteroarilo, donde grupos CY2 no vecinas también pueden estar reemplazadas por X, R1, y R3 conjuntamente también pueden significar -N-C(CF3)=N-, -N-CR=N-, -N-N=N-; Y es H, A, Hal, OR1, N(R1)2, E-R1; A es alquilo o cicloalquilo, donde uno o varios átomos de H pueden estar reemplazados por Hal y/o uno o varios grupos CH2 no vecinos pueden estar reemplazados por X; Hal es F, Cl, Br o I; R es H o A, en residuos geminales conjuntamente también -(CH2)5-, -(CH2)4-, o -(CH2)n-X-(CH2)n, o -(CH2)n-Z-(CH2)n; R4 es H ; R5 es independientemente entre sí, H o N-pirrolidona no substituida o substituida una o varias veces con OR, NO2, Hal, CF3, OCF3, CN, NR2, o SR, arilo o heteroarilo, -X-(CH2)2OR, -X-CO(CH2)nCH3, -X-(CH2)2NR2, R1, S-arilo, O-arilo, CH2Si(CH3)3, Q, -(CY2)n-E-CR2R1, -(CY2)n-E-CR2XR1, -(CY2)n-E-(CY2)n-XR1 o -(CY2)n-E-(CY2)n-XRa; E es -NR1SO2-, -SO2NR1-, - CONR1-, NR1CO-, -COO-, -OOC-, -NR1CONR1-, OCONR1-, -NR1COO-, -CSNR1-, -NR1CS-, -NR1CSNR1-, -SCONR1-, -NR1COS_, -OCSNR1-, -NR1CSO-, -SCSNR1-, -NR1CSS- o una ligadura simple; X es O, S, o NR1; Q es (CH2)pHal, CHO, CORa, (CH2)pRa, (CH2)pOCORa, (CH2)pXR1, (CH2)pNCOR1, (CH2)pN(R1)2, (CH2)pOR1, (CH2)pOCON(R1)2, (CH2)pOCOOR1, (CH2)pNHCON(R1)2, (CH2)pNHCOOR1, (CH2)pCN, (CH2)pCOOR1, (CH2)p-E-(CH2)pR1, (CH2)p-E-(CH2)pRa, donde grupos CH2 no vecinos también pueden estar reemplazados por X; o es un resto seleccionado del grupo de formulas (2); o es OR, NHR, NR2, NR(CH2)narilo, NR(CH2)nOR, COOR, N-residuo de pirrolidona, OCOR, NR(CH2)nR2, N[(CH2)nNR2]CO(CH2)narilo, N[(CH2)nNHCOOR]CO-arilo, 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)nOR, 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)nNR1COOR1, CHNR1COOR1, CHCON(R1)2, NCO, CH(CH2)nCOOR1, NCOOR1, CH(CH2)nOH, N(CH2)nOH, CHNH2, CH(CH2)nN(R1)2, C(OH)R1, CHNCOR1, NCOR1, N(CH2)narilo, N(CH2)nheteroarilo, CHR1, NR1, CH(CH2)narilo, CH(CH2)nheteroarilo, CH(CH2)nR1, N(CH2)nCOOR1, CH(CH2)nX(CH2)nR1, CH(CH2)nX(CH2)nRa, N(CH2)nCON(R1)2, XCONR1(CH2)nN(R1)2, CO(CH2)nR1, CO(CH2)nR1, CO(CH2)nXR1, SO2(CH2)nR1, O(CH2)nN(R1)2, X(CH2)nN(R1)2, NCO(CH2)nN(R1)2, CHRa, NRa; R6 es arilo o heteroarilo no substituido o substituido una o varias veces por arilo o héteroarilo, que puede estar substituido por Hal, NO2, CN, A, OR, OCOR, COR, NR2, CF3, OCF3, OCH(CF3)2, Hal, NO2, CN, OR, -(CY2)n-OR, -OCOR, -(CY2)n-CO2R, -(CY2)n-CN, -NCOR, -COR o -(CY2)n-NR2; R7 es (C=O)-R, (C=O)-NR2, (C=O)-OR, H o A, donde R5 y R7 conjuntamente también pueden significar -(CH2)n-; m es 0, 1 o 2, n es 0, 1, 2, 3, 4, 5, 6 o 7, y p es 0, 1, 2, 3, 4 o 5, preferentemente 2 o 3, s es 0, 1, 2, 3, 4, 5, 6 o 7, preferentemente 0; como así también sus derivados, solvatos, tautomeros, sales y estereoisorneros farmacéuticamente utilizables, incluyendo sus mezclas en todas las proporciones. Pueden ser utilizados, entre otros, para el tratamiento de tumores.
ARP060102410A 2005-06-13 2006-06-09 Tetrahidroquinolinas AR054615A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005027168A DE102005027168A1 (de) 2005-06-13 2005-06-13 Tetrahydrochinoline

Publications (1)

Publication Number Publication Date
AR054615A1 true AR054615A1 (es) 2007-07-04

Family

ID=36870019

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060102410A AR054615A1 (es) 2005-06-13 2006-06-09 Tetrahidroquinolinas

Country Status (15)

Country Link
US (1) US8207345B2 (es)
EP (1) EP1891011B1 (es)
JP (1) JP5420898B2 (es)
AR (1) AR054615A1 (es)
AT (1) ATE490957T1 (es)
AU (1) AU2006257414B2 (es)
CA (1) CA2611893C (es)
CY (1) CY1111432T1 (es)
DE (2) DE102005027168A1 (es)
DK (1) DK1891011T3 (es)
ES (1) ES2357625T3 (es)
PL (1) PL1891011T3 (es)
PT (1) PT1891011E (es)
SI (1) SI1891011T1 (es)
WO (1) WO2006133821A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005027170A1 (de) * 2005-06-13 2006-12-14 Merck Patent Gmbh Substituierte Tetrahydrochinoline
DE102006060598A1 (de) * 2006-12-21 2008-06-26 Merck Patent Gmbh Tetrahydrobenzoisoxazole
DE102007013854A1 (de) * 2007-03-20 2008-09-25 Merck Patent Gmbh Tetrahydrochinoline
JP5455915B2 (ja) 2007-10-19 2014-03-26 メルク・シャープ・アンド・ドーム・コーポレーション Ｋｓｐキネシン活性を阻害するためのスピロ縮合した１，３，４−チアジアゾール誘導体
JP2013075830A (ja) * 2010-02-03 2013-04-25 Taisho Pharmaceutical Co Ltd キノリン誘導体
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
CA2959208C (en) 2014-08-29 2023-09-19 Tes Pharma S.R.L. Pyrimidine derivatives and their use as inhibitors of alpha-amino-beta-carboxymuconate-epsilon-semialdehyde decarboxylase

Family Cites Families (13)

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JPH0395117A (ja) * 1989-06-13 1991-04-19 Kyorin Pharmaceut Co Ltd 代謝性骨疾患治療剤
JPH0772175B2 (ja) * 1990-09-28 1995-08-02 フアイザー・インコーポレイテツド 窒素含有非芳香族複素環の縮合環類似体
GB9216911D0 (en) * 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
EP0925300A1 (en) * 1996-02-15 1999-06-30 Cambridge Neuroscience, Inc. Pharmaceutically active compounds and methods of use
FR2760237B1 (fr) * 1997-02-28 1999-04-16 Rhone Poulenc Rorer Sa Thiazolobenzoheterocycles, leur preparation et les medicaments les contenant
WO1999067238A2 (en) * 1998-06-25 1999-12-29 Sepracor, Inc. Tetrahydroquinoline-indole derivatives antimicrobial agents, their uses and compositions containing them
JP2000072773A (ja) * 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
WO2002094788A1 (en) 2001-05-22 2002-11-28 Eli Lilly And Company 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods
ITMI20012060A1 (it) * 2001-10-05 2003-04-05 Recordati Chem Pharm Nuovi eterocilcli n-acilati
WO2004072041A1 (en) * 2003-02-12 2004-08-26 Care X S.A. Tetrahydroquinolines as agonists of liver- x receptors
DK1601673T3 (da) 2003-03-07 2009-08-24 Astrazeneca Ab Kondenserede heterocykler og anvendelser af disse
CN1194969C (zh) * 2003-05-30 2005-03-30 中国科学院大连化学物理研究所 对映选择性铱催化氢化取代芳香吡啶环和吡嗪环的方法
DE102005027170A1 (de) * 2005-06-13 2006-12-14 Merck Patent Gmbh Substituierte Tetrahydrochinoline

Also Published As

Publication number Publication date
WO2006133821A1 (de) 2006-12-21
US8207345B2 (en) 2012-06-26
AU2006257414A1 (en) 2006-12-21
PL1891011T3 (pl) 2011-05-31
ES2357625T3 (es) 2011-04-28
JP2008545805A (ja) 2008-12-18
EP1891011B1 (de) 2010-12-08
EP1891011A1 (de) 2008-02-27
CA2611893A1 (en) 2006-12-21
DE102005027168A1 (de) 2006-12-14
DK1891011T3 (da) 2011-03-21
ATE490957T1 (de) 2010-12-15
JP5420898B2 (ja) 2014-02-19
CY1111432T1 (el) 2015-08-05
DE502006008473D1 (de) 2011-01-20
US20080200451A1 (en) 2008-08-21
CA2611893C (en) 2013-12-17
AU2006257414B2 (en) 2011-08-25
PT1891011E (pt) 2011-03-11
SI1891011T1 (sl) 2011-04-29

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