PE69498A1 - PIRIDINE 3-SULFONAMIDE DERIVATIVES - Google Patents

PIRIDINE 3-SULFONAMIDE DERIVATIVES

Info

Publication number
PE69498A1
PE69498A1 PE1997000444A PE00044497A PE69498A1 PE 69498 A1 PE69498 A1 PE 69498A1 PE 1997000444 A PE1997000444 A PE 1997000444A PE 00044497 A PE00044497 A PE 00044497A PE 69498 A1 PE69498 A1 PE 69498A1
Authority
PE
Peru
Prior art keywords
compounds
cycle
preference
react
alkyl
Prior art date
Application number
PE1997000444A
Other languages
Spanish (es)
Inventor
Derek Edward Brundish
Lyndon Nigel Brown
Grand Darren Mark Le
Keith Allan Menear
Garrick Paul Smith
Mark Christopher Allen
Paul Ian Butler
Xiao-Ling Cockroft
Ian Timothy William Matthews
Clive Victor Walker
William Bernard Wathey
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 PE69498A1 publication Critical patent/PE69498A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I), EN DONDE: "A" Y R ESTAN AUSENTES o "A" ES UN GRUPO METILENO O ETILENO; R ES H, HALOGENO, AZIDA, OR9, NR10R11; R9 ES H, ALQUILO O HIDROXIALQUILO; R10 Y R11 SON H, ALQUILO O JUNTO CON EL ATOMO DE N FORMAN UN CICLO; m ES 0; 1 o 2; n ES 1; 2 o 3; R1 ES DE PREFERENCIA FENILO OPCIONALMENTE SUSTITUIDO CON UNO MAS 0R4, SR5 o NR6R7; R2 ES UN DERIVADO DE AMINOACIDO, TAL COMO FENILALANINA, TIROSINA O DOPA, ENTRE OTROS; SIENDO R2-CH2 DE PREFERENCIA 4-METILAMINOBENCILO, 2-BENZOTIAZOLILMETILO O 4-HIDROXIBENCILO, ENTRE OTROS; R3 PRESENTA 2 o 3 ATOMOS DE CARBONO Y SE ENCUENTRA OPCIONALMENTE SUSTITUIDO POR OH, F O Cl; R4, R5, R6 Y R7 SON H, ALQUILO O HETEROCICLO MONO O BICICLICO, ENTRE OTROS; EN LOS COMPUESTOS EXISTEN Y SE PREFIEREN 2 CENTROS ASIMETRICOS DE CONFIGURACIONES (S). TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LOS COMPUESTOS DE FORMULA (I), QUE COMPRENDE: 1. REACCIONAR 4-CLOROPIRIDINA-3-SULFONILCLORURO CON X-CO-CH(CH2-R2)-NH2, EN DONDE "X" ES OH, OPCIONALMENTE PROTEGIDO, 2. REACCIONAR LO OBTENIDO EN (1) CON R1(CH2)m-CH(NH2)-A-R, 3. REACCIONAR LO OBTENIDO EN (2) CON UNA BASE DE AMINA CICLICA. LOS COMPUESTOS OBTENIDOS ACTUAN COMO INHIBIDORES POTENTES DE LAS PROTEASAS DE SERINA (TROMBINA), TIENEN BUENA BIODISPONIBILIDAD Y SON USADOS EN EL TRATAMIENTO DE TROMBOSIS DE VENA, ENTRE OTROSTHEY REFER TO COMPOUNDS OF FORMULA (I), WHERE: "A" AND R ARE ABSENT or "A" IS A METHYLENE OR ETHYLENE GROUP; R IS H, HALOGEN, AZIDA, OR9, NR10R11; R9 IS H, ALKYL OR HYDROXIALKYL; R10 AND R11 ARE H, RENT OR TOGETHER WITH THE ATOM OF N FORM A CYCLE; m IS 0; 1 or 2; n IS 1; 2 or 3; R1 IS OF PREFERENCE FENILE OPTIONALLY REPLACED WITH ONE MORE 0R4, SR5 or NR6R7; R2 IS A DERIVATIVE OF AMINO ACID, SUCH AS PHENYLALANINE, THYROSINE OR DOPA, AMONG OTHERS; PREFERENCE R2-CH2 BEING 4-METHYLAMINOBENCIL, 2-BENZOTIAZOLYLMETHYLL OR 4-HYDROXYBENCIL, AMONG OTHERS; R3 PRESENTS 2 or 3 CARBON ATOMS AND IS OPTIONALLY REPLACED BY OH, F OR Cl; R4, R5, R6 AND R7 ARE H, ALKYL OR HETERO-CYCLE MONO OR BICYCLE, AMONG OTHERS; IN THE COMPOUNDS THERE ARE 2 ASYMMETRIC CONFIGURATION CENTERS AND ARE PREFERRED (S). IT ALSO REFERS TO THE PROCEDURE FOR THE PREPARATION OF FORMULA (I) COMPOUNDS, WHICH INCLUDES: 1. REACTION 4-CHLOROPYRIDINE-3-SULPHONYL CHLORIDE WITH X-CO-CH (CH2-R2) -NH2, WHERE "X" IS OH , OPTIONALLY PROTECTED, 2. REACT THE OBTAINED IN (1) WITH R1 (CH2) m-CH (NH2) -AR, 3. REACT THE OBTAINED IN (2) WITH A CYCLE AMINE BASE. THE COMPOUNDS OBTAINED ACT AS POWERFUL INHIBITORS OF SERINE PROTEASES (THROMBINE), HAVE GOOD BIOAVAILABILITY AND ARE USED IN THE TREATMENT OF VENOMINE THROMBOSIS, AMONG OTHERS

PE1997000444A 1996-06-01 1997-05-29 PIRIDINE 3-SULFONAMIDE DERIVATIVES PE69498A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9611461.6A GB9611461D0 (en) 1996-06-01 1996-06-01 New compounds

Publications (1)

Publication Number Publication Date
PE69498A1 true PE69498A1 (en) 1998-11-27

Family

ID=10794610

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000444A PE69498A1 (en) 1996-06-01 1997-05-29 PIRIDINE 3-SULFONAMIDE DERIVATIVES

Country Status (8)

Country Link
AR (1) AR008376A1 (en)
AU (1) AU2908197A (en)
CO (1) CO4940504A1 (en)
GB (1) GB9611461D0 (en)
ID (1) ID16990A (en)
PE (1) PE69498A1 (en)
WO (1) WO1997046553A1 (en)
ZA (1) ZA974779B (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040007672A (en) * 2001-06-12 2004-01-24 에스케이 주식회사 Novel Phenylalkyl Diamine and Amide Analogs
CA2462200A1 (en) * 2001-08-10 2003-02-20 Palatin Technologies, Inc. Peptidomimetics of biologically active metallopeptides
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CA2725140A1 (en) * 2008-05-22 2009-11-26 Boehringer Ingelheim International Gmbh Alpha-substituted n-sulfonyl gylcine amides antagonists of ccr10, compositions containing the same and methods for using them
EP2640367A2 (en) 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
WO2012071509A2 (en) 2010-11-24 2012-05-31 Exelixis, Inc. Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
CN112679448B (en) * 2020-12-31 2022-08-19 苏州昊帆生物股份有限公司 Preparation method of N- (2-aminoethyl) morpholine

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH31294A (en) * 1992-02-13 1998-07-06 Thomae Gmbh Dr K Benzimidazolyl derivatives, pharmaceutical compositions containing these compounds and process for preparing them.
CA2150550A1 (en) * 1992-12-01 1994-06-09 Melissa S. Egbertson Fibrinogen receptor antagonists
FR2727413B1 (en) * 1994-11-25 1996-12-20 Synthelabo DERIVATIVES OF 5- (1H-IMIDAZOL-4-YL) -1-OXO-2- (PHENYLSULFONAMINO) - PENTYLPIPERIDINE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Also Published As

Publication number Publication date
ZA974779B (en) 1997-12-01
AR008376A1 (en) 2000-01-19
CO4940504A1 (en) 2000-07-24
WO1997046553A1 (en) 1997-12-11
GB9611461D0 (en) 1996-08-07
ID16990A (en) 1997-11-27
AU2908197A (en) 1998-01-05

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