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AR048032A1 - Compuestos de bifenilo utiles como antagonistas de receptores muscarinicos, un proceso para su preparacion, composiciones farmaceuticas que los contienen, su uso en la fabricacion de un medicamento para el tratamiento de afecciones pulmonares y un metodo para estudiar una muestra biologica que los c - Google Patents

Compuestos de bifenilo utiles como antagonistas de receptores muscarinicos, un proceso para su preparacion, composiciones farmaceuticas que los contienen, su uso en la fabricacion de un medicamento para el tratamiento de afecciones pulmonares y un metodo para estudiar una muestra biologica que los c

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Publication number
AR048032A1
AR048032A1 ARP050100927A ARP050100927A AR048032A1 AR 048032 A1 AR048032 A1 AR 048032A1 AR P050100927 A ARP050100927 A AR P050100927A AR P050100927 A ARP050100927 A AR P050100927A AR 048032 A1 AR048032 A1 AR 048032A1
Authority
AR
Argentina
Prior art keywords
compound
formula
alkyl
compounds
reacting
Prior art date
Application number
ARP050100927A
Other languages
English (en)
Inventor
Mathai Mammen
Yu-Hua Ji
Yong Qi Mu
Craig Husfeld
Original Assignee
Theravance 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 Theravance Inc filed Critical Theravance Inc
Publication of AR048032A1 publication Critical patent/AR048032A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A61K9/124—Aerosols; Foams characterised by the propellant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • A61P13/06—Anti-spasmodics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Los compuestos de la formula (1) son antagonistas del receptor muscarínico. Composiciones farmacéuticas que contienen dichos compuestos, procesos e intermediarios para preparar dichos compuestos y métodos para utilizar de dichos compuestos para tratar afecciones pulmonares. Reivindicacion 1: Un compuesto de la formula (1), donde: a es 0 o un entero entre 1 y 5; cada R1 se selecciona en forma independiente entre C1-4 alquilo, C2-4 alquenilo, C2-4 alquinilo, C3-6 cicloalquilo, ciano, halo, - OR1a, -C(O)OR1b, -SR1c, -S(O)R1d, -S(O)2R1e y -NR1fR1g; donde cada uno de R1a, R1b, R1c, R1d, R1e, R1f y R1g es en forma independiente hidrogeno, C1-4 alquilo o fenil-C1-4alquilo; b es 0 o un entero entre 1 y 4; cada R2 se selecciona en forma independiente entre C1-4 alquilo, C2-4 alquenilo, C2-4 alquinilo, C3-6 cicloalquilo, ciano, halo, -OR2a, -C(O)OR2b, -SR2c, -S(O)R2d, -S(O)2R2e y -NR2fR2g; donde cada uno de R2a, R2b, R2c, R2d, R2e, R2f y R2g es en forma independiente hidrogeno, C1-4 alquilo o fenil-C1-4alquilo; W representa O o NWa, donde Wa es hidrogeno o C1-4 alquilo; c es 0 o un entero entre 1 y 5; cada R3 representa en forma independiente C1-4 o dos grupos R3 se unen para formar C1-3 alquileno, C2-3 alquenileno o oxiran-2,3- diilo; m es 0 o 1; R4 es hidrogeno o C1-4 alquilo; s es 0, 1 o 2; Ar1 representa un grupo fenileno o un grupo C3-5 heteroarileno que contienen 1 o 2 heteroátomos seleccionados en forma independiente entre oxígeno, nitrogeno o azufre; donde el anillo fenileno o heteroarileno está sustituido con (R5)q donde q es 0 o un entero entre 1 y 4 y cada R5 se selecciona independiente entre halo, hidroxi, C1-4 alquilo o C1-4 alcoxi; t es 0, 1 o 2; n es 0, 1 o 2: d es 0 o un entero entre 1 y 4; cada R6 representa en froam independiente fluoro o C1-4 alquilo; p es 0 o 1; R7 y R8 son en forma independiente hidrogeno o C1-4 alquilo; donde cada grupo alquilo y alcoxi en R1, R1a-1g, R2, R2a-2g, R3, R5, R6, R7 o R8 está sustituido opcionalmente con entre 1 y 5 sustituyentes fluoro; o una sal o un solvato o un estereoisomero aceptables para uso farmacéutico del mismo. Reivindicacion 18: Un proceso para preparar un compuesto de cualquiera de las reivindicaciones 1 y 14, caracterizada porque comprende: a) hacer reaccionar un compuesto de la formula (2), o una sal del mismo, con un compuesto de la formula (3), donde Z1 representa un grupo saliente, o b) acoplar un compuesto de la formula (4), con un compuesto de la formula (5), o un derivado reactivo del mismo; o c) hacer reaccionar un compuesto de la formula (6), donde Z2 representa un grupo saliente; con un compuesto de la formula (7); d) hacer reaccionar un compuesto de la formula (2) con un compuesto de la formula (8), en presencia de un agente reductor; o e) hacer reaccionar un compuesto de la formula (9), con un compuesto de la formula (7) en presencia de un agente reductor; o f) hacer reaccionar un compuesto de la formula (10), donde R' es H, -CH3 o -CH2CH3, con un compuesto de la formula: NHR7R8 para dar un compuesto de la formula (1). Reivindicacion 21: Un método para estudiar un sistema o muestra biologica caracterizado porque comprende un receptor muscarínico, que comprende: a) poner en contacto el sistema o muestra biologica con un compuesto de las reivindicaciones 1 a 14; y b) determinar los efectos causados por el compuesto en el sistema o muestra biologica.
ARP050100927A 2004-03-11 2005-03-10 Compuestos de bifenilo utiles como antagonistas de receptores muscarinicos, un proceso para su preparacion, composiciones farmaceuticas que los contienen, su uso en la fabricacion de un medicamento para el tratamiento de afecciones pulmonares y un metodo para estudiar una muestra biologica que los c AR048032A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US55244304P 2004-03-11 2004-03-11

Publications (1)

Publication Number Publication Date
AR048032A1 true AR048032A1 (es) 2006-03-22

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Application Number Title Priority Date Filing Date
ARP050100927A AR048032A1 (es) 2004-03-11 2005-03-10 Compuestos de bifenilo utiles como antagonistas de receptores muscarinicos, un proceso para su preparacion, composiciones farmaceuticas que los contienen, su uso en la fabricacion de un medicamento para el tratamiento de afecciones pulmonares y un metodo para estudiar una muestra biologica que los c
ARP160101213A AR104444A2 (es) 2004-03-11 2016-04-28 Derivado de ácido bifenil carbámico y sus sales

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ARP160101213A AR104444A2 (es) 2004-03-11 2016-04-28 Derivado de ácido bifenil carbámico y sus sales

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US (22) US7288657B2 (es)
EP (2) EP1723114B1 (es)
JP (1) JP4837653B2 (es)
KR (1) KR101174740B1 (es)
CN (1) CN1930125B (es)
AR (2) AR048032A1 (es)
AT (2) ATE467617T1 (es)
AU (1) AU2005222411B2 (es)
BR (1) BRPI0508622B8 (es)
CA (1) CA2557479C (es)
CY (1) CY1109015T1 (es)
DE (2) DE602005021258D1 (es)
DK (1) DK1723114T3 (es)
ES (2) ES2345640T3 (es)
HR (1) HRP20080301T3 (es)
IL (1) IL177359A (es)
MA (1) MA28524B1 (es)
MY (1) MY144482A (es)
NO (1) NO338941B1 (es)
NZ (1) NZ549472A (es)
PL (1) PL1723114T3 (es)
PT (1) PT1723114E (es)
RU (1) RU2366656C2 (es)
SI (1) SI1723114T1 (es)
TW (1) TWI341836B (es)
WO (1) WO2005087738A1 (es)
ZA (1) ZA200607099B (es)

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