AR079934A1 - Derivados de carbamato de alquil -heterociclos, su preparacion y su aplicacion en terapeutica - Google Patents

Derivados de carbamato de alquil -heterociclos, su preparacion y su aplicacion en terapeutica

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Publication number
AR079934A1
AR079934A1 ARP110100169A ARP110100169A AR079934A1 AR 079934 A1 AR079934 A1 AR 079934A1 AR P110100169 A ARP110100169 A AR P110100169A AR P110100169 A ARP110100169 A AR P110100169A AR 079934 A1 AR079934 A1 AR 079934A1
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AR
Argentina
Prior art keywords
group
alkylene
cycle
alkyl
representing
Prior art date
Application number
ARP110100169A
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English (en)
Inventor
Ahmed Abouabdellah
Antoine Ravet
Original Assignee
Sanofi Aventis
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
Priority claimed from FR1050362A external-priority patent/FR2955325B1/fr
Priority claimed from FR1050583A external-priority patent/FR2955580A1/fr
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR079934A1 publication Critical patent/AR079934A1/es

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    • 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
    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Neurosurgery (AREA)
  • Neurology (AREA)
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  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Otolaryngology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composicion farmacéutica, como moduladores de la enzima FAAH. Reivindicacion 1: Compuesto que responde a la formula general (1) en la que R2 representa un átomo de hidrogeno, fluor o un grupo hidroxilo, ciano, trifluorometilo, alquilo C1-6, alcoxi C1-6, -NR8R9; representando n y m independientemente entre sí un numero entero igual a 1, 2 o 3, entendiéndose que la suma m+n es como máximo igual a 5; A representa un enlace covalente, un átomo de oxígeno, un grupo alquileno C1-6 o un grupo -O-alquileno C1-6 en el que el extremo representado por un átomo de oxígeno está unido al grupo R1; R1 representa un grupo R5 sustituido opcionalmente por uno o varios grupos R6 y/o R7; representado R5 un grupo elegido entre un fenilo, piridinilo, piridazinilo, pirimidinilo, pirazinilo, triazinilo, naftalenilo, quinolinilo, isoquinolinilo, ftalazinilo, quinazolinilo, quinoxalinilo, cinnolinilo, naftiridinilo, benzotiazolilo, benzoisotiazolilo, benzoxazolilo, benzoisoxazolilo, benzoimidazolilo, isobenzofuranilo, benzofuranilo, benzotiofenilo, benzotiadiazolilo, benzoxadiazolilo, indazolilo, indolizinilo, indolilo, isoindolilo, imidazopiridinilo, imidazopirimidinilo, imidazopirazinilo, imidazopiridazinilo, triazolopiridinilo, pirrolopiridinilo pirrolopirimidinilo, pirrolopirazinilo, pirrolopiridazinilo, pirrolotriazinilo, pirazolopiridinilo, pirazolopirimidinilo, pirazolopirazinilo, pirazolopiridazinilo, furopiridinilo, furopirimidinilo, furopirazinilo, furopiridazinilo, furotriazinilo, oxazolopiridinilo, oxazolopirimidinilo, oxazolopirazinilo, oxazolopiridazinilo, isoxazolopiridinilo, isoxazolopirimidinilo, isoxazolopirazinilo, isoxazolopiridazinilo, oxadiazolopiridinilo, tienopiridinilo, tienopirimidinilo, tienopirazinilo, tienopiridazinilo, tienotriazinilo, tiazolopiridinilo, tiazolopirimidinilo, tiazolopirazinilo, tiazolopiridazinilo, isotiazolopiridinilo, isotiazolopirimidinilo, isotiazolopirazinilo, isotiazolopiridazinilo, tiadiazolopiridinilo; representando R6 un átomo de halogeno, un grupo ciano, -CH2CN, nitro, hidroxilo, alquilo C1-8, alcoxi C1-6, tioalquilo C1-6, haloalquilo C1-6, haloalcoxi C1-6, halotioalquilo C1-6, cicloalquilo C3-7, cicloalquilo C3-7-alquileno C1-3, cicloalquilo C3-7-alquileno-C1-3-O-, -(CH2)p-NR8R9, -NR8COR9, -NR8CO2R9, -NR8SO2R9, -NR8SO2NR8R9, -COR8, -CO2R8, -(CH2)p-CONR8R9, -SO2R8, -SO2NR8R9 o -O-(alquileno C1-3)-O-; representando R7 un grupo elegido entre un fenilo, fenilo-alquileno C1-4-, fenilo-(CH2)p-O-, piridinilo, piridazinilo, pirimidinilo, pirazinilo, triazinilo, furanilo, tienilo, imidazolilo, oxazolilo, isoxazolilo, pirrolilo, pirazolilo, tetrazolilo, tiazolilo, isotiazolilo, oxadiazolilo, tiadazolilo, imidazopirimidinilo, tienopirimidinilo, benzofuranilo, benzotienilo, benzimidazolilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, indolilo, isoindolilo, indazolilo, pirrolopiridinilo, furopiridinilo, tienopiridinilo, imidazopiridinilo, pirazolopiridinilo, oxazolopiridinilo, isoxazolopiridinilo, tiazolopiridinilo; pudiendo estar el o los grupos R7 sustituidos por uno o varios grupos R6 idénticos o diferentes entre sí; representando p un numero que puede tener el valor 0, 1, 2 o 3; R3 representa un átomo de hidrogeno, fluor, un grupo alquilo C1-6 o un grupo trifluorometilo; R4 representa un heterociclo de 5-eslabones elegido entre un furanilo, pirrolilo, tienilo, tiazolilo, isotiazolilo, oxazolilo, isoxazolilo, pirrazolilo, oxadiazolilo, tiadiazolilo, imidazol, triazolilo, tetrazolilo; estando este heterociclo opcionalmente sustituido con uno o varios sustituyentes elegidos entre un átomo de halogeno, un grupo alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7, cicloalquilo C3-7-alquileno C1-3, haloalcoxi C1-6, ciano, -NR8R9, -NR8C(O)R9, -NR8CO2R9, -NR8SO2R9, -NR8SO2NR8R9, -C(O)R8, -CO2R8, -C(O)NR8R9, -C(O)N(R8)(alquileno C1-3-NR10R11), -SO2R8, -SO2NR8R9, -O-(alquileno C1-3)-O-; representando R8 y R9 independientemente entre sí un átomo de hidrogeno o un grupo alquilo C1-6 o forman con el o los átomos de nitrogeno que les llevan, en el caso de NR8R9, un ciclo elegido entre los ciclos: azetidina, pirrolidina, piperidina, morfolina, tiomorfolina, azepina, oxazepina o piperazina, estando este ciclo sustituido opcionalmente por un grupo alquilo C1-6 o bencilo; en el caso de NR8COR9, un ciclo lactama; en el caso de NR8CO2R9, un ciclo oxazolidinona, oxacinona u oxazepinona; en el caso de NR8SO2R9, un ciclo sultama; en el caso de NR8SO2NR8R9, un ciclo dioxido de tiazolidina o dioxido de tiadiazinano; representando R10 y R11 independientemente entre sí un átomo de hidrogeno o un grupo alquilo C1-6 con exclusion del compuesto siguiente: 4-hidroxi-4-(4-cloro-fenil)-piperidin-1-carboxilato de 5-metil-isoxazol-3-ilmetilo, en forma de base o de sal de adicion a un ácido.
ARP110100169A 2010-01-20 2011-01-19 Derivados de carbamato de alquil -heterociclos, su preparacion y su aplicacion en terapeutica AR079934A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1050362A FR2955325B1 (fr) 2010-01-20 2010-01-20 Derives de carbamates d'alkyl-heterocycles, leur preparation et leur application en therapeutique
FR1050583A FR2955580A1 (fr) 2010-01-28 2010-01-28 Derives de carbamate d'alkyl-heterocycles, leur preparation et leur application en therapeutique

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AR079934A1 true AR079934A1 (es) 2012-02-29

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EP (1) EP2526100B1 (es)
JP (1) JP5833570B2 (es)
KR (1) KR20120125302A (es)
CN (2) CN102803258B (es)
AR (1) AR079934A1 (es)
AU (1) AU2011208418B2 (es)
CA (1) CA2787476C (es)
IL (1) IL220859A0 (es)
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WO2018068295A1 (en) * 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. ARYL AND HETEROARYL ETHER DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE

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CA2787476A1 (en) 2011-07-28
CN102803258B (zh) 2016-04-20
US9000010B2 (en) 2015-04-07
KR20120125302A (ko) 2012-11-14
EP2526100A1 (en) 2012-11-28
CN105837565A (zh) 2016-08-10
RU2012135525A (ru) 2014-02-27
CA2787476C (en) 2017-07-11
AU2011208418A1 (en) 2012-08-09
TW201139431A (en) 2011-11-16
WO2011089550A1 (en) 2011-07-28
CN102803258A (zh) 2012-11-28
US20120295909A1 (en) 2012-11-22
EP2526100B1 (en) 2013-12-04
MX2012008377A (es) 2012-12-05
AU2011208418B2 (en) 2016-01-07
JP2013517323A (ja) 2013-05-16

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