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PE20040938A1 - Compuestos (2-carboxamido)(3-amino)tiofenos - Google Patents

Compuestos (2-carboxamido)(3-amino)tiofenos

Info

Publication number
PE20040938A1
PE20040938A1 PE2004000046A PE2004000046A PE20040938A1 PE 20040938 A1 PE20040938 A1 PE 20040938A1 PE 2004000046 A PE2004000046 A PE 2004000046A PE 2004000046 A PE2004000046 A PE 2004000046A PE 20040938 A1 PE20040938 A1 PE 20040938A1
Authority
PE
Peru
Prior art keywords
amino
carboxamide
thiofen
compounds
ilmethyl
Prior art date
Application number
PE2004000046A
Other languages
English (en)
Inventor
Kevin Doyle
Graham Michael Wynne
An-Hu Li
Chrystelle Marie Rasamison
Imaad Saba
Don Smyth
Gary Newton
Crew Andrew Phillip
Arlindo Lucas Castelhiano
Graham Dawson
Shazia Sadiq
Claire Thomas
Neil Anthony Pegg
John Fraser Keily
Saleh Ahmed
Original Assignee
Osi Pharm Inc
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 Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of PE20040938A1 publication Critical patent/PE20040938A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A COMPUESTOS (2-CARBOXAMIDO)(3-AMINO)TIOFENOS DE FORMULA I DONDE R1 ES EL GRUPO a, ENTRE OTROS; R2 ES EL GRUPO b, ENTRE OTROS. SON COMPUESTOS PREFERIDOS N-(4-TRIFLUOROMETOXIFENIL)-3-[(QUINOLIN-4-ILMETIL)AMINO]TIOFEN-2-CARBOXAMIDA, N-(4-BROMO-3-METILFENIL)-3-[(QUINOLIN-4-ILMETIL)AMINO]TIOFEN-2-CARBOXAMIDA, N-(2,2,3,3-TETRAFLUOROBENZODIOXAN-6-IL)-3-[(QUINOLIN-4-ILMETIL)AMINO]TIOFEN-2-CARBOXAMIDA, N-(4-CLOROFENIL)-3-[(QUINOLIN-4-ILMETIL)AMINO]TIOFEN-2-CARBOXAMIDA, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DEL PROTO-ONCOGEN c-kit (CD-117 RECEPTOR DEL FACTOR DE CELULAS TRONCALES, RECEPTOR DEL FACTOR DE CRECIMIENTO DE MASTOCITOS) Y SON UTILES PARA EL TRATAMIENTO DEL CANCER
PE2004000046A 2003-01-06 2004-01-06 Compuestos (2-carboxamido)(3-amino)tiofenos PE20040938A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43815203P 2003-01-06 2003-01-06
US52497203P 2003-11-25 2003-11-25
US52635803P 2003-12-02 2003-12-02

Publications (1)

Publication Number Publication Date
PE20040938A1 true PE20040938A1 (es) 2004-12-27

Family

ID=32719185

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000046A PE20040938A1 (es) 2003-01-06 2004-01-06 Compuestos (2-carboxamido)(3-amino)tiofenos

Country Status (14)

Country Link
US (3) US6949563B2 (es)
EP (1) EP1590328B1 (es)
JP (1) JP4685755B2 (es)
KR (1) KR101017140B1 (es)
AR (1) AR042706A1 (es)
AT (1) ATE546435T1 (es)
BR (1) BRPI0406646A (es)
CA (1) CA2512608C (es)
ES (1) ES2379874T3 (es)
LV (1) LV13360B (es)
MX (1) MXPA05007296A (es)
PE (1) PE20040938A1 (es)
TW (1) TWI299664B (es)
WO (1) WO2004063330A2 (es)

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TWI299664B (en) * 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
ATE453628T1 (de) * 2004-04-01 2010-01-15 Rexahn Pharmaceuticals Inc Nucleosidderivate und deren therapeutische verwendung
WO2006023707A2 (en) * 2004-08-20 2006-03-02 Bayer Pharmaceuticals Corporation 2-aminothiophenecarboxamides useful as cancer chemotherapeutic agents
WO2006034075A1 (en) * 2004-09-17 2006-03-30 Osi Pharmaceuticals, Inc. (hydrazido) (amino) thiophene compounds
WO2006034015A1 (en) * 2004-09-17 2006-03-30 Osi Pharmaceuticals, Inc. (spirocyclylamido) aminothiophene compounds as c-kit proto- oncogene inhibitors
US7618965B2 (en) * 2004-09-17 2009-11-17 Osi Pharmaceuticals, Inc. (Arylamidoanilino)nitroethylene compounds
KR20070118100A (ko) * 2005-03-04 2007-12-13 바이엘 파마슈티칼스 코포레이션 암 화학요법제로서 유용한 1,3-티아졸-5-카르복사미드
WO2007028145A2 (en) * 2005-09-02 2007-03-08 Dara Biosciences, Inc. Agents and methods for reducing protein tyrosine phosphatase 1b activity in the central nervous system
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JP2011504926A (ja) * 2007-11-28 2011-02-17 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド Egfrキナーゼ阻害剤とc−kit阻害剤による併用治療
WO2010088000A2 (en) * 2009-02-02 2010-08-05 Angion Biomedica Corp. Antifibrotic compounds and uses thereof
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Also Published As

Publication number Publication date
CA2512608A1 (en) 2004-07-29
CA2512608C (en) 2011-06-28
LV13360B (en) 2006-01-20
US20050192320A1 (en) 2005-09-01
JP4685755B2 (ja) 2011-05-18
WO2004063330A2 (en) 2004-07-29
AR042706A1 (es) 2005-06-29
JP2007524571A (ja) 2007-08-30
EP1590328B1 (en) 2012-02-22
AU2004204135A1 (en) 2004-07-29
EP1590328A2 (en) 2005-11-02
US6949563B2 (en) 2005-09-27
WO2004063330A3 (en) 2005-02-17
EP1590328A4 (en) 2007-09-19
KR20050114210A (ko) 2005-12-05
ES2379874T3 (es) 2012-05-04
BRPI0406646A (pt) 2005-12-06
US20040186124A1 (en) 2004-09-23
ATE546435T1 (de) 2012-03-15
US20060247275A1 (en) 2006-11-02
TW200503712A (en) 2005-02-01
US7101893B2 (en) 2006-09-05
US7524859B2 (en) 2009-04-28
KR101017140B1 (ko) 2011-02-25
MXPA05007296A (es) 2005-09-30
TWI299664B (en) 2008-08-11

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