AR055273A1 - Pi3-quinasas, sus usos y composiciones farmaceuticas que los contienen - Google Patents

Pi3-quinasas, sus usos y composiciones farmaceuticas que los contienen

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Publication number
AR055273A1
AR055273A1 ARP050104225A ARP050104225A AR055273A1 AR 055273 A1 AR055273 A1 AR 055273A1 AR P050104225 A ARP050104225 A AR P050104225A AR P050104225 A ARP050104225 A AR P050104225A AR 055273 A1 AR055273 A1 AR 055273A1
Authority
AR
Argentina
Prior art keywords
alkyl
het
alkenyl
aryl
nitrogen
Prior art date
Application number
ARP050104225A
Other languages
English (en)
Inventor
Steffen Breitfelder
Udo Maier
Trixi Brandl
Christoph Hoenke
Matthias Grauert
Alexander Pautsch
Matthias Hoffmann
Frank Kalkbrenner
Anne Joergensen
Gerhard Schaenzle
Stefan Petters
Eckhart Bauer
Frank Buettner
Original Assignee
Boehringer Ingelheim Int
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
Priority claimed from DE102004048877A external-priority patent/DE102004048877A1/de
Priority claimed from DE102005005813A external-priority patent/DE102005005813A1/de
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR055273A1 publication Critical patent/AR055273A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/84Naphthothiazoles

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Debido a su accion farmacéutica como moduladores de la PI3-quinasa pueden utilizarse en el área terapéutica para el tratamiento de enfermedades inflamatorias o alérgicas. A modo de ejemplo, se mencionan enfermedades inflamatorias o alérgicas de las vías respiratorias, enfermedades inflamatorias del tracto gastro-intestinal, artritis reumatoidea, patologías dérmicas inflamatorias y alérgicas, patologías oftálmicas inflamatorias, patologías de la mucosa nasal, estados patologicas inflamatorios o alérgicos, en los cuales inciden reacciones autoinmunes o inflamaciones renales. Reivindicacion 1: Compuestos de formula (1), con la condicion, que la línea circular identificada con A significa un sistema aromático; donde Y significa carbono, átomo de nitrogeno, azufre; de preferencial carbono, nitrogeno; Z significa carbono, nitrogeno, azufre; de preferencia carbono, nitrogeno; j 1, 2 o 3; k 0 o 1; Ra es H, COR8, NR9R10, NO2, OR8, SR11, SOR11, SO2R11, NHCO-alquiloC1-6-NH2, o un radical seleccionado del grupo que incluye alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, cicloalquenilo C3-8, haloalquilo C1-6, arilo, aralquilo C7-11, espiro, Het, heteroarilo y CH2-O-arilo, que en su caso puede estar sustituido; R8 significa alquilo C1- 6, cicloalquilo C3-6, NH2, hetarilo o arilo, en su caso sustituido con uno o varios halogenos o alquilo C1-4; R9 significa H, COOR12, CONR12 o alquilo C1-6, en su caso sustituido con uno o varios COOH, N(alquilo C1-6)2 o Het, en su caso sustituido con uno o varios alquilo C1-6; o R9 significa Het, en su caso sustituido con uno o varios alquilo C1-4; R10 significa H, alquilo C1-6, CO-alquiloC1-6 o alquinilo C2-6; R11 significa alquilo C1-6, en su caso sustituido con uno o varios N(alquilo C1- 4)2; Rb es R4, OR4, -CH2OR4, COR4, COOR4, CONR4R5, NR4R5, NR5COR4, NR5COOR4, NR5CONR4R5, NR5SOR4 o NR5SO2R4; R4, R5 significan H, alquilo C1-6, haloalquilo C1-6, alquileno C1-6-OH, alquenilo C2-6, aralquilo C7-11, alqueniloC2-4-arilo, alquiniloC2-4- arilo, alquiloC1-4-hetarilo, alqueniloC2-4-hetarilo, alquiniloC2-4-hetarilo, alquinilo C2-6, en su caso sustituido con Si(alquilo C1-4)3, o R4 significa un radical seleccionado del grupo que incluye arilo, Het, Hetarilo y en su caso alquilo C1-4; o R4 y R5 forman conjuntamente un anillo de cinco, seis o siete miembros que se compone de átomo de carbono y en su caso un heteroátomo seleccionado del grupo que se compone de oxígeno, nitrogeno y azufre; Rc significa NHR6 o un radical seleccionado del grupo que incluye la formula (2) donde: B significa un enlace, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; R6 es H o un radical seleccionado del grupo alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, cicloalquenilo C3-6, Het, arilo, hetarilo en su caso sustituido con uno o varios radicales R6,1; R6,1 es halogeno, CF3, OH, CN, OMe, SO2(alquilo C1-4); R7 significa H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, NR7,1R7,2, OR7,2, SR7,2, hetarilo, Het, en su caso sustituido con alquilo C1-4 o CONH2; R7,1 significa H, alquilo C1-6, (CH2)2-4R7,1,1 o COO-butilo; R7,2 significa H, alquilo C1-6, en su caso sustituido con uno o varios OH; R7,1,1NR7,1,1,1R7,1,1,2, Het o 1-imidazolilo, 2-(N-etilpirrolidina); R7,1,1,1 es H o alquilo C1-6; R7,1,1,2 es H o alquilo C1-6; así como sales aceptables para uso farmacéuticos, diaesteromeros, enantiomeros, racematos, hidratos o solvatos de éstos, con la condicion, que Ra no puede ser H o Me, cuando significan Y = nitrogeno; Z = nitrogeno; j = 2; k = 0; Rb= H y Rc = NHCONH-Et.
ARP050104225A 2004-10-07 2005-10-07 Pi3-quinasas, sus usos y composiciones farmaceuticas que los contienen AR055273A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004048877A DE102004048877A1 (de) 2004-10-07 2004-10-07 PI3-Kinasen
DE102005005813A DE102005005813A1 (de) 2005-02-09 2005-02-09 PI3-Kinasen

Publications (1)

Publication Number Publication Date
AR055273A1 true AR055273A1 (es) 2007-08-15

Family

ID=35583390

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050104225A AR055273A1 (es) 2004-10-07 2005-10-07 Pi3-quinasas, sus usos y composiciones farmaceuticas que los contienen

Country Status (14)

Country Link
US (4) US7691888B2 (es)
EP (2) EP2343303A1 (es)
JP (1) JP5122287B2 (es)
KR (1) KR20070064660A (es)
CN (1) CN101048418A (es)
AR (1) AR055273A1 (es)
AU (1) AU2005293607A1 (es)
BR (1) BRPI0516557A (es)
CA (1) CA2579279C (es)
IL (1) IL182398A0 (es)
MX (1) MX2007004051A (es)
RU (2) RU2007116861A (es)
TW (1) TW200628475A (es)
WO (1) WO2006040279A1 (es)

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JP2008515852A (ja) 2008-05-15
CA2579279A1 (en) 2006-04-20
EP1802636B1 (de) 2013-03-27
EP2343303A1 (de) 2011-07-13
US8207349B2 (en) 2012-06-26
RU2007116861A (ru) 2009-03-20
MX2007004051A (es) 2007-05-24
TW200628475A (en) 2006-08-16
RU2007116858A (ru) 2008-12-27
AU2005293607A1 (en) 2006-04-20
RU2403258C2 (ru) 2010-11-10
US8232286B2 (en) 2012-07-31
US20060106013A1 (en) 2006-05-18
EP1802636A1 (de) 2007-07-04
WO2006040279A1 (de) 2006-04-20
US20090156554A1 (en) 2009-06-18
CA2579279C (en) 2013-10-01
IL182398A0 (en) 2007-07-24
BRPI0516557A (pt) 2008-09-09
US20100113414A1 (en) 2010-05-06
US20060100254A1 (en) 2006-05-11
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JP5122287B2 (ja) 2013-01-16
US7691888B2 (en) 2010-04-06

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