AR040074A1 - Tiazolidinonas, su preparacion y su uso como medicamentos, e intermediarios para la preparacion de dichos compuestos - Google Patents

Tiazolidinonas, su preparacion y su uso como medicamentos, e intermediarios para la preparacion de dichos compuestos

Info

Publication number
AR040074A1
AR040074A1 ARP030101572A ARP030101572A AR040074A1 AR 040074 A1 AR040074 A1 AR 040074A1 AR P030101572 A ARP030101572 A AR P030101572A AR P030101572 A ARP030101572 A AR P030101572A AR 040074 A1 AR040074 A1 AR 040074A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkylene
cycloalkyl
group
aryl
Prior art date
Application number
ARP030101572A
Other languages
English (en)
Inventor
Eis Knut Dr
Buchmann Bernd Dr
Briem Hans Dr
Gerhard Siemeister
Boemer Ulf Dr
Schawede Wolfgang Dr
Schulze Volker Dr
Original Assignee
Schering 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 Schering Ag filed Critical Schering Ag
Publication of AR040074A1 publication Critical patent/AR040074A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/34—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • 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
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Tiazolidonas de la fórmula general (1), preparación de un medicamento en base al compuesto y su uso como inhibidores de la cinasa tipo polo (PLK) para el tratamiento de diversas enfermedades; así como productos intermediarios para preparar las tiazolidonas. Estos compuestos son inhibidores de la cinasa tipo polo (PLK) y se aplican en el tratamiento de ciertas enfermedades, especialmente las tumorales. Reivindicación 1: Compuestos de la fórmula general (1) donde: X e Y son iguales o diferentes y son hidrógeno, arilo, ciano, cicloalquilo C3-6 o el grupo -COOR4, -CONR15-(CH2)n-R25, -COOR25, -CONR15R16 o -COR13; R1, R11, R12, R15, R16, R19 y R20 son iguales o diferentes y son hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, (COOR14)-(CH2)n-, cicloalquil (C3-6)-alquileno (C1-4), cicloalquilo C3-6, fenilsulfonilo, fenil-cicloalquilo C3-6, alcanoilo C1-10, alcoxi(C1-6)-alquileno(C1-6), alcoxicarbonil(C1-4)-alquileno(C1-4), hidroxi-alquileno C1-4, alquil (C1-6)-O-Si(fenil)2-alquilo (C1-6), o el grupo COOR14, -COR13, -SO2R18, -(CH2)n-NR15R16 o -(CH2)n-C(CH3)q-(CH2)nNR15R16 o -NR11R12, o un grupo del resto de fórmulas (2), o son, arilo, heteroarilo, heterociclilo, aril-alquileno (C1-4), heteroaril-alquileno C1-4, ariloxi-alquileno C1-4, heteroariloxi-alquileno C1-4 o aril-alquilenoxi(C1-4)-alquileno(C1-4) opcionalmente mono o polisustituido, igual o diferente, por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, cicloalquiloxi C3-6, fenilo, ciano, halógeno, hidroxi, alcoxi C1-4, fenoxi, benciloxi, alquilsulfanilo C1-4, bencilsulfanilo, fenilsulfanilo, dimetilamino, acetilamino, trifluorometilo, trifluorometoxi, trifluorometilsulfanilo, acetilo, -CO-alquilo C1-6, 1-iminoetilo o nitro, o alquilo C1-10 mono o polisustituido por flúor; R2 y R3 son iguales o diferentes y son hidrógeno, alquilo C1-6, hidroxi-alquileno C1-6, ciclohexilo C3-6 o el grupo -COOR14, -CONR15R16, -COR13, -SO2R18, -NR11R12, -(CH2)n-A, o un resto de fórmula (3) y (4), o arilo, heteroarilo o heterociclilo opcionalmente mono o polisustituido, igual o diferente, por alquilo C1-6, cicloalquilo C3-6, halo-alquilo C1-6, halo-alcoxi C1-6, halógeno, ciano, hidroxi-alquileno C1-6, hidroxi-alquilenoxi C1-6, arilo, heteroarilo, heterociclilo, alquil(C1-6)-COOR8 o por el grupo -OR10, -COR13, -COOR14, -NR11R12, -NR11-CO-NR11R12, -NR11-CO-R13, -NR11-SO2-R13, -(CH2)n-CO-NR15R16, -SR10 o -SO2R18; R4, R8, R9, R10, R13, R14, R17 y R18 son iguales o diferentes y son hidrógeno, alquilo C1-10, hidroxi-alquilenoxi(C1-6)-alquileno(C1-6), alcoxi(C1-6)-CO-alquileno(C1-6), -(CH2)n-CO-NR15R16, alquenilo C2-10, alquinilo C2-10, cicloalquil (C3-6)-alquileno(C1-4), halo-alquilo C1-6, hidroxi-alquileno C1-6, (COOR14)-(CH2)n-, hidroxi-(CH2)n-O-(CH2)n, cicloalquilo C3-6, alcanoilo C1-10, o el grupo -NR11R12, -(CH2)n-CO-R25, -(CH2)n-NR15R16, COOR14-(CH2)n- o -COR13, o arilo, heteroarilo, heterociclilo, aril-alquileno C1-4, heteroaril-alquileno C14, ariloxi-alquileno C1-4, heteroariloxi-alquileno C1-4 o aril-alquilenoxi(C1-4)-alquileno(C1-4) opcionalmente mono o polisustituido, igual o diferente, por alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, cicloalquiloxi C3-6, fenilo, ciano, halógeno, hidroxi-alquilo C1-6, alcoxi C1-4, fenoxi, benciloxi, alquilsulfanilo C1-4, bencilsulfanilo, fenilsulfanilo, dimetilamino, acetil-amino, trifluorometilo, trifluorometoxi, trifluorometilsulfanilo, acetilo, -CO-alquilo C1-6, 1-iminoetilo o nitro, o alquilo C1-10 mono o polisustituido por flúor o el grupo -NR11R12, -COR13, -SO2R18, -(CH2)n-NR15R16, -(CH2)n-C(CH3)q-(CH2)nR15R16 o un grupo de resto de fórmula (2), o R2 y R3, R11 y R12, R15 y R16 y R19 y R20 forman cada uno, independientemente entre sí, un anillo de 3 a 10 miembros, que puede contener opcionalmente uno o varios átomos de nitrógeno, oxígeno o azufre; o R3 es hidrógeno y R2 es el grupo -(L-M), donde L es un grupo -C(O)-, -S(O)2-, -C(O)N(R7)-, -S(O)2 n(R7)-, -C(S)N(R7)-, C(S)N(R7)C(O)O-, -C(O)O- o -C(O)S- y M es hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquil(C3-6)-alquileno(C1-4), cicloalquilo C3-6, fenil-cicloalquilo C3-6, alcanoilo C1-10, alcoxi(C1-4)-alquileno(C1-4), alcoxicarbonil(C1-4)-alquileno(C1-4), hidroxialquileno C1-10, o arilo, heteroarilo, heterociclilo, aril-alquileno C1-4, heteroaril-alquileno C1-4, ariloxi-alquileno C1-4, heteroariloxi-alquileno C1-4 o aril-alquilenoxi(C1-4)-alquileno(C1-4) opcionalmente mono o polisustituido, igual o diferente, por alquilo C1-4, alquenilo C2-6, cicloalquilo C3-6, cicloalquiloxi C3-6, fenilo, ciano, halógeno, fenoxi, benciloxi, halo-alcoxi C1-4, halo-alquilo C1-6, nitro, alquil C1-6-COOR8, alquenil C2-6-COOR8, alquinil C2-6-COOR8, alquil C1-6-OR9, alquenil C2-6-OR9, alquinil C1-6-OR9 o por el grupo -OR10, -NR11R12, -COR13, -COOR14, -CONR15R16, -SR17, -SO2R18, SO2NR19R20 o -C(NH)(NH2), o un alquilo C1-10 mono o polisustituido por flúor; y R7 es hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-6, (cicloalquil C3-6)-alquileno C1-4, aril-alquileno C1-4; A es arilo, heteroarilo o heterociclilo opcionalmente sustituido; R22 es hidrógeno, hidroxi-alquilo C1-6, o es el grupo -OR10, -NR11R12, -COR13, -CONR15R16, -SO2R18, -NR15-(C=S)-NR16-(CH2)n-R24, -NR15-(C=O)-NR16-(CH2)n-R24; R23 es hidrógeno o alquilo C1-6; R24 es hidrógeno, fenilo, alcoxi C1-6 o el grupo -(CH2)n-COO-alquilo C1-6; R25 el grupo -OR10 o alquenilo C2-6, fenilo, piridilo, imidazolilo, morfolinilo, piperidinilo, cicloalquilo C3-6 o un restos de fórmula (5) opcionalmente mono o polisustituido, igual o diferente, por halógeno, alquilo C1-6, hidroxi-alquilo C1-6 o por el grupo -OR10 o -COOR14; o m, p, k son cada uno, independientemente entre sí 0 ó 1; n es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 ó 10; q es 1 ó 2, así como los estereoisómeros, las mezclas de los estereoisómeros y las sales de los mismos.
ARP030101572A 2002-05-03 2003-05-05 Tiazolidinonas, su preparacion y su uso como medicamentos, e intermediarios para la preparacion de dichos compuestos AR040074A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10221104 2002-05-03

Publications (1)

Publication Number Publication Date
AR040074A1 true AR040074A1 (es) 2005-03-16

Family

ID=29285317

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101572A AR040074A1 (es) 2002-05-03 2003-05-05 Tiazolidinonas, su preparacion y su uso como medicamentos, e intermediarios para la preparacion de dichos compuestos

Country Status (21)

Country Link
US (1) US20060079503A1 (es)
EP (1) EP1501794A1 (es)
JP (1) JP2005538048A (es)
KR (1) KR20040106451A (es)
CN (1) CN1649853A (es)
AR (1) AR040074A1 (es)
AU (1) AU2003222845A1 (es)
BR (1) BR0309758A (es)
CA (1) CA2484597A1 (es)
EC (1) ECSP045476A (es)
HR (1) HRP20041142A2 (es)
IL (1) IL164651A0 (es)
MX (1) MXPA04010169A (es)
NO (1) NO20045281L (es)
PE (1) PE20040589A1 (es)
PL (1) PL372890A1 (es)
RS (1) RS95404A (es)
RU (1) RU2004135533A (es)
TW (1) TW200406392A (es)
WO (1) WO2003093249A1 (es)
ZA (1) ZA200409796B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
DE10351744A1 (de) 2003-10-31 2005-06-16 Schering Ag Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
DE102004033670A1 (de) * 2004-07-09 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7759485B2 (en) * 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US7728134B2 (en) * 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
EP1630163A1 (de) 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1632493A1 (de) * 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE102004058337A1 (de) * 2004-12-02 2006-06-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten
DE102004061503A1 (de) * 2004-12-15 2006-06-29 Schering Ag Metasubstituierte Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
WO2006063806A1 (de) * 2004-12-15 2006-06-22 Bayer Schering Pharma Aktiengesellschaft Metasubstituierte thiazolidinone, deren herstellung und verwendung als arzneimittel
CA2590939C (en) * 2004-12-17 2011-10-18 Amgen Inc. Aminopyrimidine compounds and methods of use
DE102005005395A1 (de) * 2005-02-03 2006-08-10 Schering Aktiengesellschaft Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
US7297700B2 (en) 2005-03-24 2007-11-20 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
DE102005020104A1 (de) * 2005-04-25 2006-10-26 Schering Ag Neue Thiazolidinone ohne basischen Stickstoff, deren Herstellung und Verwendung als Arzneimittel
DE102005020105A1 (de) * 2005-04-25 2006-10-26 Schering Ag Neue Thiazolidinone ohne basischen Stickstoff, deren Herstellung und Verwendung als Arzneimittel
US20070010565A1 (en) * 2005-04-25 2007-01-11 Olaf Prien New thiazolidinones without basic nitrogen, their production and use as pharmaceutical agents
EP1989330A4 (en) * 2006-01-31 2009-10-21 Elan Pharm Inc ALPHA-SYNUCLEINE KINASE
US7439358B2 (en) 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
TWI464148B (zh) 2006-03-16 2014-12-11 Evotec Us Inc 作為ｐ２ｘ7調節劑之雙環雜芳基化合物與其用途
EP2124562B1 (en) 2007-03-09 2016-04-20 Second Genome, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
WO2009019205A1 (en) 2007-08-03 2009-02-12 Boehringer Ingelheim International Gmbh Crystalline form of a dihydropteridione derivative
EP2247748A2 (en) * 2008-02-13 2010-11-10 Elan Pharma International Limited Alpha-synuclein kinase
EP2100894A1 (en) 2008-03-12 2009-09-16 4Sc Ag Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors
EP2141163A1 (de) * 2008-07-02 2010-01-06 Bayer Schering Pharma AG Substituierte Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
CA2745596A1 (en) 2008-12-18 2010-10-28 F. Hoffmann-La Roche Ag Thiazolyl-benzimidazoles
CN101780074B (zh) * 2010-03-02 2011-11-16 山东大学 一种抗肺癌的药物组合物
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
WO2014069434A1 (ja) * 2012-10-30 2014-05-08 カルナバイオサイエンス株式会社 新規チアゾリジノン誘導体
US20150031699A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
RU2546006C1 (ru) * 2014-03-07 2015-04-10 Римма Ильинична Ашкинази Противовирусное средство
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
US10080728B2 (en) 2015-01-20 2018-09-25 Viktor Veniaminovich Tets Hemostatic agent
WO2018217743A1 (en) 2017-05-24 2018-11-29 Viktor Veniaminovich Tets Fractionated antimicrobial compositions and use thereof
CN113788814B (zh) * 2021-10-15 2022-07-01 云南省烟草质量监督检测站 稻瘟灵含量检测用半抗原、制备方法及其应用
CN114380976B (zh) * 2022-01-13 2024-02-06 西安恩诺维新石油技术有限公司 一种油田用缓释型荧光示踪覆膜支撑剂及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6016989A (ja) * 1983-07-06 1985-01-28 Shionogi & Co Ltd オキソ飽和異項環カルボンアミドセフエム化合物
MXPA01012442A (es) * 1999-06-03 2004-09-10 Abbott Gmbh & Co Kg Compuestos de benzotiazinona y benzoxazinona.
US6291496B1 (en) * 1999-12-27 2001-09-18 Andrew J. Dannenberg Treating cancers associated with overexpression of class I family of receptor tyrosine kinases
DE102005005395A1 (de) * 2005-02-03 2006-08-10 Schering Aktiengesellschaft Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel

Also Published As

Publication number Publication date
JP2005538048A (ja) 2005-12-15
EP1501794A1 (de) 2005-02-02
CN1649853A (zh) 2005-08-03
AU2003222845A1 (en) 2003-11-17
RU2004135533A (ru) 2005-07-20
WO2003093249A1 (de) 2003-11-13
NO20045281L (no) 2005-02-01
KR20040106451A (ko) 2004-12-17
CA2484597A1 (en) 2003-11-13
PL372890A1 (en) 2005-08-08
BR0309758A (pt) 2005-02-15
PE20040589A1 (es) 2004-11-21
RS95404A (en) 2006-10-27
TW200406392A (en) 2004-05-01
MXPA04010169A (es) 2005-02-03
HRP20041142A2 (en) 2005-10-31
ECSP045476A (es) 2005-01-28
IL164651A0 (en) 2005-12-18
ZA200409796B (es) 2006-06-28
US20060079503A1 (en) 2006-04-13

Similar Documents

Publication Publication Date Title
AR040074A1 (es) Tiazolidinonas, su preparacion y su uso como medicamentos, e intermediarios para la preparacion de dichos compuestos
CL2004000174A1 (es) Compuestos derivados de malonamida n,n&#39;-disustituidos; procedimiento de preparacion; composicion farmaceutica; y uso del compuesto en el tratamiento de la enfermedad de alzheimer.
AR050261A2 (es) Aminoacidos con afinidad por la proteina alfa-2-delta y composiciones farmaceuticas que los contienen y su uso para preparar un medicamento
AR041566A1 (es) Derivados de indol utiles para el tratamiento de enfermedades
AR035617A1 (es) Compuestos derivados de fenetanolamina, combinaciones y formulaciones farmaceuticas de los mismos, proceso para su preparacion, su uso en la preparacion de medicamentos para el tratamiento o profilaxis de una condicion clinica para la cual se indica un agonista beta2 adreno-receptor e intermediarios
AR030324A1 (es) Derivados de 4-fenil-piridina
CO5251381A1 (es) Derivados de adamantano, un proceso para su preparacion y composiciones farmaceuticas que los contienen
AR061841A1 (es) Derivados de tiofen-oxadiazoles, agonistas del receptor s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores.
AR024060A1 (es) Nuevos compuestos farmaceuticamente activos
CO5680443A2 (es) Derivados de bencimidazol, composiciones que los contienen, preparacion de los mismos y usos de los mismos
AR033306A1 (es) Compuestos
PE20011035A1 (es) Ureas ciclicas sustituidas como antagonistas de los receptores de neuroquinina
PE20021010A1 (es) Derivados espirociclicos como inhibidores de fosfodiesterasa-7
SE0203754D0 (sv) New compounds
DOP2001000170A (es) Derivados de tiofeno utiles como agentes anticancesoros
AR035069A1 (es) Compuestos inhibidores de espiropirimidin-2,4,6-triona metaloproteinasas, composicion farmaceutica, procedimiento de tratamiento
PE20021004A1 (es) Derivados de piperidina como inhibidores de la ccr5
PE20030739A1 (es) Antagonistas del receptor de adenosina a2a
CO5640137A2 (es) N-pirazinil-fenilsulfonamidas y su uso en el tratamiento de enfermedades mediadas por quimosina
AR074148A1 (es) Derivados de corticoesteroides beta agonistas fosforilados, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades del aparato respiratorio
PE20050012A1 (es) Compuestos de benzopirano como inhibidores de la ciclooxigenasa-2
AR035254A1 (es) Derivados fluorquinolonicos de oxazolidinonas utiles como antibacterianos, procedimiento para su obtencion y su utilizacion para la preparacion de una composicion farmaceutica
AR056338A1 (es) Derivados hexahidroquinolina, composiciones farmaceuticas y su uso en el tratamiento de desordenes de fertilidad
AR057005A1 (es) Derivados de 4-fenil-5-oxo-1,4,5,6,7,8-hexahidroquinolina, una composicion farmaceutica y uso del compuesto para preparar un medicamento
AR039651A1 (es) Derivados de isoquinolina

Legal Events

Date Code Title Description
FB Suspension of granting procedure