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BR9815170A - "método de obter composto aplicável no tratamento de asma em mamìferos" - Google Patents

"método de obter composto aplicável no tratamento de asma em mamìferos"

Info

Publication number
BR9815170A
BR9815170A BR9815170-3A BR9815170A BR9815170A BR 9815170 A BR9815170 A BR 9815170A BR 9815170 A BR9815170 A BR 9815170A BR 9815170 A BR9815170 A BR 9815170A
Authority
BR
Brazil
Prior art keywords
alkyl
straight
optionally substituted
alkylene groups
compound
Prior art date
Application number
BR9815170-3A
Other languages
English (en)
Inventor
David Cavalla
Mark Chasin
Peter Hofer
Original Assignee
Euro Celtique S A Luxembourg
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 Euro Celtique S A Luxembourg filed Critical Euro Celtique S A Luxembourg
Publication of BR9815170A publication Critical patent/BR9815170A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • 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
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Compounds Of Unknown Constitution (AREA)

Abstract

Patente de invenção de "MéTODO DE OBTER COMPOSTO APLICáVEL NO TRATAMENTO DE ASMA EM MAMìFEROS". A invenção se refere mais especificamente compostos que sejam mais efetivos inibidores de PDE IV que aqueles da técnica anterior. O composto em questão apresenta a fórmula geral (I) : onde: Z é selecionado do grupo consistindo de grupos de alquileno tais como CH2, CH2CH2CH(CH3), grupos alquilenos tais como CH=CH; grupos alquileno tais como C <MU>= <MV>C ; e NH, N(C1-C3 alquila) , O,S,C(O)CH2 e OCH2; R1 e R2 são independentemente selecionados do grupo consistindo de hidrogênio e uma alquila de cadeia reta ou ramificada C1-C8 ou cicloalquila C3-C8; R3 é uma alquila de cadeia reta ou ramificada; R4 é uma cicloalquila C3-C10 opcionalmente substituída com OH ou uma cicloalquila opcionalmente substituída com OH, e R8 é uma alquila de cadeia reta ou ramificada ou uma cicloalquila C3-C8 opcionalmente substituída com OH. Segundo a invenção o composto é obtido pelas seguintes etapas: (a) reagir um composto da fórmula (II) : onde Z, R3 e R4 são como acima definido, com uma quantidade efetiva de um éster para formas um composto da fórmula (III) : onde Z é selecionado do grupo consistindo de grupos de alquileno tais como CH2, CH2CH2CH(CH3), grupos alquilenos tais como CH=CH; grupos alquileno tais como C <MU>= <MV>C ; e NH, N (C1-C3 alquila),O,S,C (O) CH2 e OCH2;R1 e R2 são independentemente selecionados do grupo consistindo de hidrogênio e uma alquila de cadeia reta ou ramificada C1-C8 ou cicloalquila C3-C8; R3 é uma alquila de cadeia reta ou ramificada; R4 é uma cicloalquila C3-C10 opcionalmente substituída com OH ou uma cicloalquila opcionalmente substituída com OH, e (b) submeter dito composto (III) a etapas sucessivas de aminação, redução e amidação para formar o composto(IV) ; onde: Z é selecionado do grupo consistindo de grupos de alquileno tais como CH2, CH2CH2CH (CH3), grupos alquilenos tais como CH=CH; grupos alquileno tais como C <MU>= <MV>C ; e NH, N(C1-C3 alquila),O,S,C (O) CH2 e OCH2; R1 e R2 são independentemente selecionados do grupo consistindo de hidrogênio e uma alquila de cadeia reta ou ramificada C1-C8 ou cicloalquila C3-C8; R3 é uma alquila de cadeia reta ou ramificada; R4 é uma cicloalquila C3-C10 opcionalmente substituída com OH ou uma cicloalquila opcionalmente substituída com OH, e R8 é uma alquila de cadeia reta ou ramificada ou uma cicloalquila C3-C8 opcionalmente substituída com OH. (.c) reagir dito composto (IV) com uma quantidade efetiva de uma base para formar o composto (V) Onde Z é selecionado do grupo consistindo de grupos de alquileno tais como CH2, CH2CH2CH(CH3), grupos alquilenos tais como CH=CH; grupos alquileno tais como C <MU>= <MV> C; e NH, N (C1-C3 alquila),O,S,C (O) CH2 e OCH2; R1 e R2 são independentemente selecionados do grupo consistindo de hidrogênio e uma alquila de cadeia reta ou ramificada C1-C8 ou cicloalquila C3-C8; R3 é uma alquila de cadeia reta ou ramificada; R4 é uma cicloalquila C3-C10 opcionalmente substituída com OH ou uma cicloalquila opcionalmente substituída com OH, e R8 é uma alquila de cadeia reta ou ramificada ou uma cicloalquila C3-C8 opcionalmente substituída com OH. (d) reagir dito composto(V) com uma quantidade efetiva de um composto de desulfuração para formar o composto (VI) : onde Z é selecionado do grupo consistindo de grupos de alquileno tais como CH2, CH2CH2CH(CH3), grupos alquilenos tais como CH=CH; grupos alquileno tais como C <MU>= MV>C ; e NH, N(C1-C3 alquila),O,S,C (O) CH2 e OCH2; R1 e R2 são independentemente selecionados do grupo consistindo de hidrogênio e uma alquila de cadeia reta ou ramificada C1-C8 ou cicloalquila C3-C8; R3 é uma alquila de cadeia reta ou ramificada; R4 é uma cicloalquila C3-C10 opcionalmente substituída com OH ou uma cicloalquila opcionalmente substituída com OH, e R8 é uma alquila de cadeia reta ou ramificada ou uma cicloalquila C3-C8 opcionalmente substituída com OH.; e (e) submeter dito composto(VI) a etapas sucessivas de halogenação e deslocamento para formar dito composto.
BR9815170-3A 1997-12-12 1998-12-10 "método de obter composto aplicável no tratamento de asma em mamìferos" BR9815170A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6937197P 1997-12-12 1997-12-12
PCT/US1998/026340 WO1999031105A1 (en) 1997-12-12 1998-12-10 3-substituted adenines via2-thioxanthines

Publications (1)

Publication Number Publication Date
BR9815170A true BR9815170A (pt) 2000-10-10

Family

ID=22088545

Family Applications (3)

Application Number Title Priority Date Filing Date
BR9815170-3A BR9815170A (pt) 1997-12-12 1998-12-10 "método de obter composto aplicável no tratamento de asma em mamìferos"
BR9815169-0A BR9815169A (pt) 1997-12-12 1998-12-11 "método para formar um composto e composto aplicável no tratamento de asma em mamìferos, composição farmacêutica, método para efetivar a inibição seletiva de pde iv em mamìferos de estado de doença e método de tratar mamìfero sofrendo de estado de doença."
BR9815171-1A BR9815171A (pt) 1997-12-12 1998-12-11 Composto inibidor de pde iv aplicável no tratamento de doenças, particularmente de asma, em mamìferos e método para tratar um paciente sofrendo estados doentios.

Family Applications After (2)

Application Number Title Priority Date Filing Date
BR9815169-0A BR9815169A (pt) 1997-12-12 1998-12-11 "método para formar um composto e composto aplicável no tratamento de asma em mamìferos, composição farmacêutica, método para efetivar a inibição seletiva de pde iv em mamìferos de estado de doença e método de tratar mamìfero sofrendo de estado de doença."
BR9815171-1A BR9815171A (pt) 1997-12-12 1998-12-11 Composto inibidor de pde iv aplicável no tratamento de doenças, particularmente de asma, em mamìferos e método para tratar um paciente sofrendo estados doentios.

Country Status (19)

Country Link
US (5) US6037470A (pt)
EP (3) EP1044201A4 (pt)
JP (5) JP2002508378A (pt)
KR (3) KR100349385B1 (pt)
CN (3) CN1294590A (pt)
AT (1) ATE244243T1 (pt)
AU (5) AU1722999A (pt)
BR (3) BR9815170A (pt)
CA (3) CA2313004A1 (pt)
DE (3) DE19882893T1 (pt)
DK (1) DK1045849T3 (pt)
ES (1) ES2202924T3 (pt)
GB (2) GB2346878B (pt)
HU (3) HUP0301166A2 (pt)
NO (1) NO20002998L (pt)
PL (1) PL341108A1 (pt)
PT (1) PT1045849E (pt)
TR (1) TR200001706T2 (pt)
WO (5) WO1999031105A1 (pt)

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US6211367B1 (en) 2001-04-03
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ATE244243T1 (de) 2003-07-15
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