PE20121390A1 - DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA - Google Patents

DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA

Info

Publication number
PE20121390A1
PE20121390A1 PE2012000506A PE2012000506A PE20121390A1 PE 20121390 A1 PE20121390 A1 PE 20121390A1 PE 2012000506 A PE2012000506 A PE 2012000506A PE 2012000506 A PE2012000506 A PE 2012000506A PE 20121390 A1 PE20121390 A1 PE 20121390A1
Authority
PE
Peru
Prior art keywords
pyrimidin
alkyl
pyrazolo
chlorobenzyl
hydroxyphenyl
Prior art date
Application number
PE2012000506A
Other languages
English (en)
Inventor
John King-Underwood
Kazuhiro Ito
Peter John Murray
George Hardy
Frederick Arthur Brookfield
Christopher John Browne
Original Assignee
Respivert Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41462531&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121390(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Respivert Ltd filed Critical Respivert Ltd
Publication of PE20121390A1 publication Critical patent/PE20121390A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C15) EN DONDE UNO O VARIOS CARBONOS PUEDEN SER REEMPLAZADOS POR UN HETEROATOMO TAL COMO O, N, ENTRE OTROS Y ESTA OPCIONALMENTE SUSTITUIDA CON HALOGENO, ARILO, HETEROARILO, ENTRE OTROS; R3a ES HIDROXILO; R3b ES H, HIDROXILO, HALO, CN, ENTRE OTROS; R4 Y R5 SON CADA UNO H O ALQUILO(C1-C3); X ES ARILO(C6-C10) O HETEROARILO(C5-C9) SUSTITUIDO CON R2a Y R2b, EN DONDE R2a ES H, ALQUILO(C1-C3), HALO, CN, ENTRE OTROS; R2b ES H, ALQUILO(C1-C3), HALO, HALOALQUILO(C1-C3). SON COMPUESTOS PREFERIDOS: 2-((4-AMINO-3-(3-HIDROXIFENIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-IL)METIL)-3-(2-CLOROBENCIL)-5-ETINILQUINAZOLIN-4(3H)-ONA; 6-(2-((4-AMINO-3-(4-HIDROXIFENIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-IL)METIL)-3-(2-CLOROBENCIL)-4-OXO-3,4-DIHIDROQUINAZOLIN-5-IL)HEX-5-INOICO; 2-ACETAMIDO-N-(3-(2-((4-AMINO-3-(3-HIDROXIFENIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-IL)METIL)-3-(2-CLOROBENCIL)-4-OXO-3,4-DIHIDROQUINAZOLIN-5-IL)PROP-2-IN-1-IL)ACETAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE FOSFOINOSITIDA 3-QUINASAS (PI3 QUINASAS) SIENDO UTILES EN EL TRATAMIENTO DE ASMA, FIBROSIS QUISTICA, SINUSITIS, DERMATITIS ALERGICA
PE2012000506A 2009-10-19 2010-10-19 DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA PE20121390A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0918249.4A GB0918249D0 (en) 2009-10-19 2009-10-19 Compounds

Publications (1)

Publication Number Publication Date
PE20121390A1 true PE20121390A1 (es) 2012-10-15

Family

ID=41462531

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000506A PE20121390A1 (es) 2009-10-19 2010-10-19 DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA

Country Status (35)

Country Link
US (4) US8741909B2 (es)
EP (1) EP2491037B1 (es)
JP (1) JP5889792B2 (es)
KR (1) KR101770616B1 (es)
CN (1) CN102712645B (es)
AR (1) AR078674A1 (es)
AU (1) AU2010309832B2 (es)
BR (1) BR112012009214A2 (es)
CA (1) CA2777902C (es)
CL (1) CL2012000981A1 (es)
CR (1) CR20120264A (es)
CY (1) CY1116057T1 (es)
DK (1) DK2491037T3 (es)
EA (1) EA020330B3 (es)
EC (1) ECSP12011805A (es)
ES (1) ES2477270T3 (es)
GB (1) GB0918249D0 (es)
HK (1) HK1173728A1 (es)
HR (1) HRP20140599T1 (es)
IL (1) IL219248A (es)
ME (1) ME02064B (es)
MX (1) MX2012004525A (es)
MY (1) MY164731A (es)
NI (2) NI201200061A (es)
NZ (2) NZ599162A (es)
PE (1) PE20121390A1 (es)
PL (1) PL2491037T3 (es)
PT (1) PT2491037E (es)
RS (1) RS53385B (es)
SI (1) SI2491037T1 (es)
SM (1) SMT201400086B (es)
TW (1) TWI478923B (es)
UA (1) UA108743C2 (es)
WO (1) WO2011048111A1 (es)
ZA (1) ZA201203662B (es)

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