AR091534A1 - Derivados de sulfonamida y metodos de uso de los mismos para mejorar la farmacocinetica de un farmaco - Google Patents

Derivados de sulfonamida y metodos de uso de los mismos para mejorar la farmacocinetica de un farmaco

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Publication number
AR091534A1
AR091534A1 ARP130102212A ARP130102212A AR091534A1 AR 091534 A1 AR091534 A1 AR 091534A1 AR P130102212 A ARP130102212 A AR P130102212A AR P130102212 A ARP130102212 A AR P130102212A AR 091534 A1 AR091534 A1 AR 091534A1
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AR
Argentina
Prior art keywords
group
alkyl
membered
optionally substituted
alkylene
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ARP130102212A
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English (en)
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Merck Sharp & Dohme
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Publication of AR091534A1 publication Critical patent/AR091534A1/es

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    • 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
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/495—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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • C07D471/10—Spiro-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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones que comprenden al menos un derivado de sulfonamida y a métodos de uso de los derivados de sulfonamida para mejorar la farmacocinética de un fármaco. Reivindicación 1: Un compuesto que tiene la fórmula (1), o a una sal farmacéuticamente aceptable del mismo, en la que: A es un grupo heteroarilo de 5 ó 6 miembros; W es N o -CH-; X es N o -C(R³)-; R¹ está seleccionado de entre -(alquilen C₁₋₆)-arilo, -(alquilen C₁₋₆)-(heteroarilo de 5 ó 6 miembros), -(alquilen C₁₋₆)-O-arilo, -(alquilen C₁₋₆)-O-(heteroarilo de 5 ó 6 miembros) y cicloalquilo C₃₋₆, en el que cualquier grupo arilo, heteroarilo o cicloalquilo C₃₋₆ puede estar opcionalmente sustituido con hasta cuatro grupos R⁷, que pueden ser iguales o diferentes, y en el que dicho grupo cicloalquilo C₃₋₆ puede estar condensado a un anillo de benceno y dicho anillo de benceno condensado puede estar opcionalmente sustituido con hasta cuatro grupos R⁷, que pueden ser iguales o diferentes; cada aparición de R² está seleccionada independientemente de entre H, alquilo C₁₋₆, -OH, -O-(alquilo C₁₋₆) y -(alquilen C₁₋₆)-O-(alquilo C₁₋₆); R³ está seleccionado de entre H, alquilo C₁₋₆, hidroxialquilo C₁₋₆ y -CN, o R³ y un grupo R², junto con los átomos de carbono a los que están unidos, se pueden combinar para formar un anillo de ciclopropilo; R⁴ es H, o R⁴ y un grupo R², pueden formar conjuntamente un grupo seleccionado de entre -CH₂-CH₂-CH₂-, -C(O)-O-CH₂-, -CH₂-O-CH₂- y -CH₂-N(R⁸)-CH₂-; R⁵ es -NH(R⁶), heterocicloalquilo monocíclico de 5 ó 6 miembros, heterocicloalquilo bicíclico de 9 ó 10 miembros, en el que dicho grupo heterocicloalquilo monocíclico de 5 ó 6 miembros puede formar opcionalmente un espirociclo con un grupo cicloalquilo C₃₋₆ u otro grupo heterocicloalquilo monocíclico de 5 ó 6 miembros, y en el que dicho grupo heterocicloalquilo monocíclico de 5 ó 6 miembros y dicho grupo heterocicloalquilo bicíclico de 9 ó 10 miembros puede estar opcionalmente sustituido en uno o más átomos de carbono del anillo con hasta cuatro grupos R⁷, que pueden ser iguales o diferentes, y en el que un átomo de carbono del anillo de un grupo heterocicloalquilo monocíclico de 5 ó 6 miembros puede tener funcionalidad de grupo carbonilo; R⁶ es un alquilo C₁₋₆ o heteroarilo de 5 ó 6 miembros, en el que dicho grupo alquilo C₁₋₆ está opcionalmente sustituido con 1 ó 2 grupos, siendo cada uno independientemente NH₂ o halo, y en el que dicho grupo heteroarilo de 5 ó 6 miembros puede estar opcionalmente sustituido con hasta cuatro grupos R⁷; cada aparición de R⁷ está seleccionada independientemente de entre alquilo C₁₋₆, heterocicloalquilo de 5 ó 6 miembros, hidroxialquilo C₁₋₆, haloalquilo C₁₋₆, halo, -CN, -N(R⁸)₂, -CH₂N(R⁸)₂, -OR⁸, -C(O)OR⁸, -SR⁸, -S(O)₂R⁸ y -C(O)N(R⁸)₂, en el que dicho grupo heterocicloalquilo de 5 ó 6 miembros puede estar opcionalmente sustituido con un grupo seleccionado de entre alquilo C₁₋₆, halo, hidroxialquilo C₁₋₆, haloalquilo C₁₋₆, halo, -CN, -N(R⁸)₂ y -OR⁸; y cada aparición de R⁸ es independientemente H o alquilo C₁₋₆.
ARP130102212A 2012-06-27 2013-06-24 Derivados de sulfonamida y metodos de uso de los mismos para mejorar la farmacocinetica de un farmaco AR091534A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2012/077611 WO2014000178A1 (en) 2012-06-27 2012-06-27 Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug

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AR091534A1 true AR091534A1 (es) 2015-02-11

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ARP130102212A AR091534A1 (es) 2012-06-27 2013-06-24 Derivados de sulfonamida y metodos de uso de los mismos para mejorar la farmacocinetica de un farmaco

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US (2) US9556202B2 (es)
EP (1) EP2867220B1 (es)
JP (1) JP2015522021A (es)
AR (1) AR091534A1 (es)
AU (1) AU2013280599A1 (es)
CA (1) CA2876240A1 (es)
TW (1) TW201406749A (es)
WO (2) WO2014000178A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014000178A1 (en) * 2012-06-27 2014-01-03 Merck Sharp & Dohme Corp. Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug
WO2015070367A1 (en) * 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Piperidine or piperazine linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
KR20230109185A (ko) 2016-06-07 2023-07-19 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
US10988466B2 (en) 2017-03-23 2021-04-27 Jacobio Pharmaceuticals Co., Ltd. Heterocyclic derivatives useful as SHP2 inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60320957D1 (en) * 2002-03-13 2008-06-26 Janssen Pharmaceutica Nv Sulfonylderivate als histone-deacetylase-inhibitoren
AR053845A1 (es) * 2005-04-15 2007-05-23 Tibotec Pharm Ltd 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450
PL1937639T3 (pl) 2005-09-23 2010-07-30 Pfizer Prod Inc Pirydynoaminosulfonylo podstawione benzamidy jako inhibitory cytochromu p450 3a4 (cyp3a4)
AP2009004763A0 (en) 2006-07-05 2009-02-28 Pfizer Prod Inc Pyrazole derivatives as cytochrome P450 inhibitors
NZ573060A (en) * 2006-07-07 2012-02-24 Gilead Sciences Inc Modulators of pharmacokinetic properties of therapeutics
WO2009088719A1 (en) 2008-01-04 2009-07-16 Gilead Sciences, Inc. Inhibitors of cytochrome p450
WO2014000178A1 (en) * 2012-06-27 2014-01-03 Merck Sharp & Dohme Corp. Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug

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JP2015522021A (ja) 2015-08-03
AU2013280599A1 (en) 2014-12-18
WO2014000178A1 (en) 2014-01-03
EP2867220A1 (en) 2015-05-06
EP2867220B1 (en) 2016-12-14
WO2014004416A1 (en) 2014-01-03
US20150197531A1 (en) 2015-07-16
TW201406749A (zh) 2014-02-16
US20140005103A1 (en) 2014-01-02
CA2876240A1 (en) 2014-01-03

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