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HUP0301315A2 - Benzotiazolszármazékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Benzotiazolszármazékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0301315A2
HUP0301315A2 HU0301315A HUP0301315A HUP0301315A2 HU P0301315 A2 HUP0301315 A2 HU P0301315A2 HU 0301315 A HU0301315 A HU 0301315A HU P0301315 A HUP0301315 A HU P0301315A HU P0301315 A2 HUP0301315 A2 HU P0301315A2
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Hungary
Prior art keywords
group
lower alkyl
alkyl
optionally
substituted
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Application number
HU0301315A
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English (en)
Inventor
Alexander Alanine
Alexander Flohr
Aubry Kern Miller
Roger David Norcross
Claus Riemer
Original Assignee
F. Hoffmann-La Roche Ag.
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Application filed by F. Hoffmann-La Roche Ag. filed Critical F. Hoffmann-La Roche Ag.
Publication of HUP0301315A2 publication Critical patent/HUP0301315A2/hu
Publication of HUP0301315A3 publication Critical patent/HUP0301315A3/hu

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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

A találmány tárgya (I) általános képletű vegyületek[mely képletben R1jelentése hidrogénatom, kis szénatomszámú alkil-, kis szénatomszámúalkoxi-, benziloxi-, cikloalkoxi-csoport, halogénatom, hidroxil- vagytrifluor-metoxi-csoport; R2 és R3 jelentése egymástól függetlenülhidrogénatom, halogénatom, kis szénatomszámú alkil- vagy kisszénatomszámú alkoxicsoport; R4 jelentése hidrogénatom, kisszénatomszámú alkil-, kis szénatomszámú alkenilcsoport, halogénatom, -C(O)OH, -C(O)-kis szénatomszámú alkil-, -C(O)-halogén-(kisszénatomszámú alkil)-, -CH(OH)-halogén-(kis szénatomszámú alkil)-, -C(O)O-kis szénatomszámú alkil-, -NHC(O)-kis szénatomszámú alkil-, -(CH2)n-OH csoport; vagy adott esetben a benzolgyűrűhöz -(O)m-(CH2)nlinkercsoporton keresztül kapcsolódó és adott esetben N(R5)(R6)-csoporttal, halogénatommal, alkoxi- vagy nitrocsoporttalhelyettesített fenilcsoport; vagy 2,3-dihidro-1H-indolil-csoport,azepan-1-il-csoport,[1,4]oxazepin-4-il-csoport; vagy 5- vagy 6-tagúaromás vagy nem aromás heterociklus, amely a benzolgyűrűhöz -(O)m-(CH2)n vagy -N=C(CH3)- linkercsoporton keresztül kapcsolódhat és adottesetben egy vagy két R7 csoporttal helyettesítve lehet, ahol R7jelentése a továbbiak során megadott; R jelentése a) fenilcsoport,amely adott esetben többek között kis szénatomszámú alkil-, halogén-(kis szénatomszámú alkil)-, kis szénatomszámú alkoxi-, ciano-, nitro-,formil-, karboxilcsoporttal b) CH2)n 5-vagy 6-tagú aromás vagy nemaromás heterociklus, az n = 0 esetben a piperazinilcsoportkivételével, amely gyűrű adott esetben egy vagy két szubsztituensselhelyettesítve lehet, c) adott esetben kis szénatomszámú alkoxi- vagy -N-{R5)C(O)-fenil-csoporttal helyettesített -N(R5)(CH2)n fenilcsoport;vagy d) -N(R5)(CH2)n-5-vagy 6-tagú aromás vagy nem aromásheterociklus, amely adott esetben kis szénatomszámú alkilcsoporttalhelyettesítve lehet, -(CH2)n- -5- vagy 6-tagú aromás vagy nem aromásheterociklus; vagy e) -N(R5)(CH2)n-O-kis szénatomszámú alkil-, -N(R5)(CH2)nOH, -N(R5)(CH2)nN(R5)(R6), -(CH2)nOH, oktahidro-kinolin,3,4-dihidro-1H-izokinolin, 2,3-benzo-1,4-dioxa-8-aza-spiro[4,5]dekánvagy 1,4-dioxa-8-aza-spiro[4,5]dekán; X jelentése oxigénatom; kénatom vagy két hidrogénatom; R5 és R6jelentése egymástól függetlenül hidrogénatom, vagy kis szénatomszámúalkilcsoport; R7 jelentése kis szénatomszámú alkil-, kis szénatomszámúalkoxi-csoport, -C(O)-kis szénatomszámú alkil-, -C(O)O-benzil-, -C(O)O-kis szénatomszámú alkil-, -(CH2)nNR5R6 csoport, adott esetbenkis szénatomszámú alkil-csoporttal helyettesített piridinilcsoport,vagy -CH2N(R5)-C(O)O-kis szénatomszámú alkil-, -NH-C(fenil)3-csoport,pirrolidinil-, piperidinil-, morfolinil-, adott esetben kisszénatomszámú alkilcsoporttal helyettesített piperazinilcsoport; nértéke 0, 1, 2, 3 vagy 4; m értéke 0 vagy 1; o értéke 0, 1, 2, 3 vagy4] és gyógyászatil
HU0301315A 2000-06-21 2001-06-08 Benzothiazole derivatives, process for their preparation, their use and pharmaceutical compositions containing them HUP0301315A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00113219 2000-06-21
PCT/EP2001/006506 WO2001097786A2 (en) 2000-06-21 2001-06-08 Benzothiazole derivatives

Publications (2)

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HUP0301315A2 true HUP0301315A2 (hu) 2003-08-28
HUP0301315A3 HUP0301315A3 (en) 2007-10-29

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US (8) US6521754B2 (hu)
EP (2) EP1797878A3 (hu)
JP (1) JP3886897B2 (hu)
KR (2) KR100526487B1 (hu)
CN (1) CN1234358C (hu)
AR (1) AR031244A1 (hu)
AT (1) ATE385794T1 (hu)
AU (2) AU2001281817B2 (hu)
BR (1) BR0112395A (hu)
CA (1) CA2413086C (hu)
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CZ (1) CZ2003182A3 (hu)
DE (1) DE60132777T2 (hu)
DK (1) DK1303272T3 (hu)
EC (1) ECSP024399A (hu)
ES (1) ES2299504T3 (hu)
HK (1) HK1058148A1 (hu)
HR (1) HRP20020962A2 (hu)
HU (1) HUP0301315A3 (hu)
IL (2) IL153278A0 (hu)
JO (1) JO2503B1 (hu)
MX (1) MXPA02012596A (hu)
MY (1) MY138352A (hu)
NO (2) NO324635B1 (hu)
NZ (1) NZ522928A (hu)
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SI (1) SI1303272T1 (hu)
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WO (1) WO2001097786A2 (hu)
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US6599901B1 (en) * 2001-11-19 2003-07-29 Hoffman-La Roche Inc. Pyridone substituted benzothiazole derivatives
MXPA04004982A (es) * 2001-11-27 2004-08-11 Hoffmann La Roche Derivados de benzotiazol.
US6624163B2 (en) 2001-11-29 2003-09-23 Hoffman-La Roche Inc. Benzothiazole derivatives
US6727247B2 (en) 2001-12-10 2004-04-27 Hoffman-La Roche Inc. Substituted benzothiazole amide derivatives
US6734179B2 (en) 2001-12-12 2004-05-11 Hoffmann-La Roche Inc. Benzothiazoles
DE60230808D1 (de) * 2001-12-12 2009-02-26 Hoffmann La Roche Benzothiophene als adenosinrezeptormodulatoren
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