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AR081064A1 - Compuestos de tetraciclina policiclica - Google Patents

Compuestos de tetraciclina policiclica

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Publication number
AR081064A1
AR081064A1 ARP110101090A ARP110101090A AR081064A1 AR 081064 A1 AR081064 A1 AR 081064A1 AR P110101090 A ARP110101090 A AR P110101090A AR P110101090 A ARP110101090 A AR P110101090A AR 081064 A1 AR081064 A1 AR 081064A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
alkylene
carbocyclyl
substituted
Prior art date
Application number
ARP110101090A
Other languages
English (en)
Original Assignee
Tetraphase Pharmaceuticals 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 Tetraphase Pharmaceuticals Inc filed Critical Tetraphase Pharmaceuticals Inc
Publication of AR081064A1 publication Critical patent/AR081064A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Purification Treatments By Anaerobic Or Anaerobic And Aerobic Bacteria Or Animals (AREA)

Abstract

También se describe una composicion farmacéutica que comprende el compuesto de la Formula Estructural (1) y su uso terapéutico para infecciones bacterianas. Reivindicacion 1: Un compuesto de formula estructural (1) o una sal farmacéuticamente aceptable del mismo, en la que: X se selecciona entre halo, -R, -OR, -SR, -S(O)mR, -N(R)2, N(R)C(O)R, N(R)C(O)OR' y N(R)S(O)mR', en la que: cada R se selecciona independientemente entre H, alquilo (C1-6), carbociclilo o heterociclilo, o dos grupos R tomados junto con el átomo o átomos a los que están unidos forman un heterociclilo no aromático de 4-7 miembros; y R' es alquilo (C1-6), carbociclilo o heterociclilo; anillo A es un anillo heterocíclico no aromático de 5-7 miembros opcionalmente que contiene 1-2 heteroátomos seleccionados independientemente entre N, S y O además del átomo de nitrogeno indicado, donde: R1 se selecciona entre hidrogeno, -alquilo (C1-8), -alquileno (C0-6)-carbociclilo, -alquileno (C0-6)-heterociclilo, -alquileno (C1-6)-O-alquilo (C1-6), -alquileno (C2-6)-O-carbociclilo, -alquileno (C2-6)-O-heterociclilo, S(O)m-alquilo (C1-6), -S(O)m-carbociclilo, -S(O)m-heterociclilo, -alquileno (C2-4)S(O)m-carbociclilo, -alquileno (C2-4)-S(O)m-heterociclilo, -C(O)-[C(R4)(R4)]0-4-N(R2)(R3), -C(O)-alquilo (C1-6), -C(O)-heterociclilo, -C(O)-carbociclilo, -S(O)m-[C(R4)(R4)]0-4-N(R2)(R3), y S(O)m-alquileno (C1-4)-carbociclilo, -S(O)m-alquileno (C1-4)-heterociclilo, o R1 tomado junto con un átomo de anillo adyacente al átomo de nitrogeno al que R1 está unido forma un anillo heterocíclico saturado condensado al anillo A; cada uno de R2 y R3 se selecciona independientemente entre hidrogeno, alquilo (C1-8), -alquileno (C0-6)-carbociclilo, -alquileno (C0-6)-heterociclilo, -alquileno (C2-6)-O-carbociclilo, -alquileno (C2-6)-O-heterociclilo, -S(O)m-alquilo (C1-6), -S(O)m-carbociclilo, -S(O)m-heterociclilo, -alquileno (C2-4)-S(O)m-carbociclílo y -alquileno (C2-4)-S(O)m-heterociclilo; o R2 y R3, tomados junto con el átomo de nitrogeno al que están unidos forman un heterociclilo, donde el heterociclilo opcionalmente comprende de 1 a 4 heteroátomos adicionales seleccionados independientemente entre N, S y O; cada R4 se selecciona independientemente entre hidrogeno, alquilo (C1-6), carbociclilo, heterociclilo o un resto de cadena lateral de aminoácidos de origen natural, o dos R4 tomados junto con un átomo de carbono comun al que están unidos forman un carbociclo no aromático de 3-7 miembros o un heterociclilo no aromático de 4-7 miembros, donde el heterociclilo formado por dos R4 comprende de uno a tres heteroátomos seleccionados independientemente entre N, S y O; cualquier átomo de carbono sustituido en el anillo A está opcionalmente: (i) sustituido con uno a dos sustituyentes seleccionados independientemente entre -alquilo (C1-4) y -alquileno(C0-4)-carbociclilo; o (ii) sustituido con =O; (iii) tomado junto con un átomo de anillo adyacente para formar un carbocíclico de 3-7 miembros o un anillo heterociclilo saturado de 4-7 miembros; o (iv) espirocondensado a un carbociclilo saturado de 3-7 miembros; cualquier heteroátomo de N adicional en el anillo A está sustituido con hidrogeno, alquilo C1-6, carbociclilo o heterociclilo; cada alquilo o alquileno en la Formula Estructura 1 está opcional e independientemente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -OH, =O, -O-alquilo (C1-4), -alquilo (C1-4) fluoro-sustituido, -S(O)m-alquilo (C1-4) Y -N(R5)(R5); cada porcion de carbociclilo o heterociclilo de un sustituyente del anillo A o el anillo heterocíclico saturado condensado al anillo A está opcional e independientemente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -alquilo (C1-4), -OH, =O, -O-alquilo (C1-4), -alquileno (C1-4)-O-alquilo (C1-4), -alquilo (C1-4) halo-sustituido, -O-alquilo (C1-4) halo-sustituido, -C(O)-alquilo (C1-4), -C(O)-(alquilo (C1-4) fluoro-sustituido), -S(O)m-alquilo (C1-4), -N(R5)(R5) y CN; cada R5 se selecciona independientemente entre hidrogeno y alquilo (C1-4), donde cada alquilo en el grupo representado por R5 está opcional e independientemente sustituido con uno o más sustituyentes seleccionados independientemente entre -alquilo (C1-4), cicloalquilo (C3-6), halo, -OH, -O-alquilo (C1-4) y -alquileno (C1-4)-O-alquilo (C1-4); y cada m es independientemente 1 o 2, con la condicion de que cuando X sea hidrogeno, el anillo A no sea un radical bivalente sin sustituir.
ARP110101090A 2010-03-31 2011-03-31 Compuestos de tetraciclina policiclica AR081064A1 (es)

Applications Claiming Priority (1)

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US31961410P 2010-03-31 2010-03-31

Publications (1)

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AR081064A1 true AR081064A1 (es) 2012-06-06

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ARP110101090A AR081064A1 (es) 2010-03-31 2011-03-31 Compuestos de tetraciclina policiclica

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US (2) US9371283B2 (es)
EP (1) EP2552890B1 (es)
JP (2) JP5820462B2 (es)
KR (1) KR101879751B1 (es)
CN (2) CN103180295B (es)
AR (1) AR081064A1 (es)
AU (1) AU2011235176B2 (es)
BR (1) BR112012025045A2 (es)
CA (1) CA2799727C (es)
DK (1) DK2552890T3 (es)
ES (1) ES2621409T3 (es)
MX (1) MX2012011453A (es)
NZ (1) NZ603323A (es)
PL (1) PL2552890T3 (es)
SG (1) SG184372A1 (es)
TW (1) TWI592390B (es)
WO (1) WO2011123536A1 (es)

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KR20130023231A (ko) 2013-03-07
US9371283B2 (en) 2016-06-21
EP2552890A1 (en) 2013-02-06
JP2016014058A (ja) 2016-01-28
JP5820462B2 (ja) 2015-11-24
CN106008317A (zh) 2016-10-12
PL2552890T3 (pl) 2017-07-31
CN106008317B (zh) 2019-08-23
EP2552890B1 (en) 2017-01-04
MX2012011453A (es) 2013-02-15
CA2799727C (en) 2018-06-12
AU2011235176B2 (en) 2015-05-14
JP2013523761A (ja) 2013-06-17
BR112012025045A2 (pt) 2016-06-21
ES2621409T3 (es) 2017-07-04
TW201200493A (en) 2012-01-01
DK2552890T3 (en) 2017-04-03
TWI592390B (zh) 2017-07-21
WO2011123536A1 (en) 2011-10-06
US20110269714A1 (en) 2011-11-03
WO2011123536A8 (en) 2012-02-02
KR101879751B1 (ko) 2018-08-16
CA2799727A1 (en) 2011-10-06
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CN103180295A (zh) 2013-06-26
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