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AR083202A1 - Derivados de azabiciclo[3.1.0]hexano - Google Patents

Derivados de azabiciclo[3.1.0]hexano

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Publication number
AR083202A1
AR083202A1 ARP110103576A ARP110103576A AR083202A1 AR 083202 A1 AR083202 A1 AR 083202A1 AR P110103576 A ARP110103576 A AR P110103576A AR P110103576 A ARP110103576 A AR P110103576A AR 083202 A1 AR083202 A1 AR 083202A1
Authority
AR
Argentina
Prior art keywords
rnrnr
cra
heterocyclyl
heteroaryl
aryl
Prior art date
Application number
ARP110103576A
Other languages
English (en)
Inventor
Rajesh Jain
Sanjay Trehan
Jagattaran Das
Nishan Singh
Sudhir Kumar Sharma
Original Assignee
Panacea Biotec Ltd
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 Panacea Biotec Ltd filed Critical Panacea Biotec Ltd
Publication of AR083202A1 publication Critical patent/AR083202A1/es

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    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Procesos para sintetizar compuestos de fórmula (1), los derivados, las formas tautoméricas, los estereoisómeros, las formas polimórficas, las prodrogas, los metabolitos, las sales o los solvatos farmacéuticamente aceptables de éstos. También provee composiciones farmacéuticas que comprenden compuestos de fórmula (1) y métodos para tratar o prevenir uno o más trastornos del sistema nervioso central y/o periférico, preferiblemente por modulación de blancos neurológicos y/o psiquiátricos (GPCR y/o no GPCR).Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o los derivados, formas tautoméricas, isómeros, polimorfos, prodrogas, metabolitos, sales o solvatos farmacéuticamente aceptables del mismo, donde R1 representa -H, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; cada uno de los mismos puede estar opcionalmente sustituido en cualquier posición disponible con uno o más sustituyentes seleccionados entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo, -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -Cl, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN), -CORa, -CSRa, -COORa, -CSORa, -COSRa, -CONRaRb, CSNRaRb, COCORa, -CONRaNRbRc, -CSNRaNRbRc, -CSNRaRb, -NRaRb, -NRaSO2Rb, -NRaCONRbRc, -NRaCSNRbRc, -NRa(C=NRb)NRcRd, -NRaNRbRc, -NRaCORb, -NRaCSRb, -NRaCOORb, -NRaCSORb, =NORa, -ORa, -OCORa, -OCOORa, -OCONRaRb, -OCSRa, -OCSORa, -ONO2, -OCSNRaRb, -SRa, -S(O)Ra, -S(O)2Ra, -SO2NRaRb, -CRa(=NORb), -CRa(=NCOORb), -CRa(=NSORb), -CRa(=NSO2Rb), -C(=NRa)-NRbRc, -C(=NORa)-NRbRc, -CRa(=NCN), -NCRa, -P(O)RaRb, -P(O)ORaORb, -P(O)RaORb, -P(O)NRaORb, -P(O)NRaRb, -OP(O)RaRb, -NHP(O)RaRb; con la condición de que cuando R1 es heterociclilo, arilo o heteroarilo, luego dicho heterociclilo, arilo o heteroarilo no puede estar sustituido con heterociclilo; R2 representa -H, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; cada uno de los mismos puede estar opcionalmente sustituido en cualquier posición disponible con uno o más sustituyentes seleccionados entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo, -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -Cl, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN), -CORa, -CSRa, -COORa, -CSORa, -COSRa, -CONRaRb, CSNRaRb, COCORa, -CONRaNRbRc, -CSNRaNRbRc, -CSNRaRb, -NRaRb, -NRaSO2Rb, -NRaCONRbRc, -NRaCSNRbRc, -NRa(C=NRb)NRcRd, -NRaNRbRc, -NRaCORb, -NRaCSRb, -NRaCOORb, -NRaCSORb, =NORa, -ORa, -OCORa, -OCOORa, -OCONRaRb, -OCSRa, -OCSORa, -ONO2, -OCSNRaRb, -SRa, -S(O)Ra, -S(O)2Ra, -SO2NRaRb, -CRa(=NORb), -CRa(=NCOORb), -CRa(=NSORb), -CRa(=NSO2Rb), -C(=NRa)-NRbRc, -C(=NORa)-NRbRc, -CRa(=NCN), -NCRa, -P(O)RaRb, -P(O)ORaORb, -P(O)RaORb, -P(O)NRaORb, -P(O)NRaRb, -OP(O)RaRb, -NHP(O)RaRb; R3 representa -H, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; cada uno de los mismos puede estar opcionalmente sustituido en cualquier posición disponible con uno o más sustituyentes seleccionados entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo, -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -Cl, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN), -CORa, -CSRa, -COORa, -CSORa, -COSRa, -CONRaRb, CSNRaRb, COCORa, -CONRaNRbRc, -CSNRaNRbRc, -CSNRaRb, -NRaRb, -NRaSO2Rb, -NRaCONRbRc, -NRaCSNRbRc, -NRa(C=NRb)NRcRd, -NRaNRbRc, -NRaCORb, -NRaCSRb, -NRaCOORb, -NRaCSORb, =NORa, -ORa, -OCORa, -OCOORa, -OCONRaRb, -OCSRa, -OCSORa, -ONO2, -OCSNRaRb, -SRa, -S(O)Ra, -S(O)2Ra, -SO2NRaRb, -CRa(=NORb), -CRa(=NCOORb), -CRa(=NSORb), -CRa(=NSO2Rb), -C(=NRa)-NRbRc, -C(=NORa)-NRbRc, -CRa(=NCN), -NCRa, -P(O)RaRb, -P(O)ORaORb, -P(O)RaORb, -P(O)NRaORb, -P(O)NRaRb, -OP(O)RaRb, -NHP(O)RaRb; con las siguientes condiciones (a) al menos uno de R2 y R3 es arilo o heteroarilo, (b) cuando R3 es arilo o heteroarilo, luego R3 no puede estar sustituido con heterociclilo; Z representa NOR4 o NNR4R5; R4 y R5 se seleccionan en forma independiente entre -H, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; cada uno de los mismos puede estar opcionalmente sustituido en cualquier posición disponible con uno o más sustituyentes seleccionados entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo, -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -Cl, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN), -CORa, -CSRa, -COORa, -CSORa, -COSRa, -CONRaRb, CSNRaRb, COCORa, -CONRaNRbRc, -CSNRaNRbRc, -CSNRaRb, -NRaRb, -NRaSO2Rb, -NRaCONRbRc, -NRaCSNRbRc, -NRa(C=NRb)NRcRd, -NRaNRbRc, -NRaCORb, -NRaCSRb, -NRaCOORb, -NRaCSORb, =NORa, -ORa, -OCORa, -OCOORa, -OCONRaRb, -OCSRa, -OCSORa, -ONO2, -OCSNRaRb, -SRa, -S(O)Ra, -S(O)2Ra, -SO2NRaRb, -CRa(=NORb), -CRa(=NCOORb), -CRa(=NSORb), -CRa(=NSO2Rb), -C(=NRa)-NRbRc, -C(=NORa)-NRbRc, -CRa(=NCN), -NCRa, -P(O)RaRb, -P(O)ORaORb, -P(O)RaORb, -P(O)NRaORb, -P(O)NRaRb, -OP(O)RaRb, -NHP(O)RaRb; o R4 y R5 se encuentran unidos para formar un heterociclilo; con la condición de que cuando Z es NOR4, y R4 es alquilo C1-12, luego R2 no puede ser heterociclilo o heteroarilo; Ra, Rb, Rc y Rd se seleccionan en forma independiente entre -H, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -Cl, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN), donde los grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquinilo, heterociclilo, arilo y heteroarilo pueden estar opcionalmente sustituidos en cualquier posición disponible con uno o más sustituyentes seleccionados entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo, -CN, -COCN, -N3, -NO2, -OCN, -NCO, -SCN, -NCS, -OCONH2, -ONO2, -F, -CI, -Br, -I, -CO-, -CS-, -CHO, -CHS, -COOH, -COSH, -CONH2, -CONHNH2, -CSNHNH2, -CSNH2, -NH2, -NHCONH2, -NHCSNH2, -N(C=NH)NH2, -NHNH2, -NHCHO, -NHCHS, -NHCOOH, -NHCSOH, -OH, -SH, -SO3H, -CH(=NOH), -CH(=NCN); o Ra y Rb se encuentran unidos para formar un cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; o Rb y Rc se encuentran unidos para formar un cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo; o Rc y Rd se encuentran unidos para formar un cicloalquilo C3-7, cicloalquenilo C3-7, cicloalquinilo C6-8, heterociclilo, arilo, heteroarilo.
ARP110103576A 2010-09-28 2011-09-28 Derivados de azabiciclo[3.1.0]hexano AR083202A1 (es)

Applications Claiming Priority (2)

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IN2322DE2010 2010-09-28
IN1515DE2011 2011-05-26

Publications (1)

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AR083202A1 true AR083202A1 (es) 2013-02-06

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US (1) US9133116B2 (es)
EP (1) EP2621902B1 (es)
JP (1) JP2013542929A (es)
AR (1) AR083202A1 (es)
BR (1) BR112013007566A2 (es)
WO (1) WO2012042539A2 (es)

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