AR063280A1 - Uso de compuestos de espiro-oxindol como agentes terapeuticos - Google Patents
Uso de compuestos de espiro-oxindol como agentes terapeuticosInfo
- Publication number
- AR063280A1 AR063280A1 ARP070104540A ARP070104540A AR063280A1 AR 063280 A1 AR063280 A1 AR 063280A1 AR P070104540 A ARP070104540 A AR P070104540A AR P070104540 A ARP070104540 A AR P070104540A AR 063280 A1 AR063280 A1 AR 063280A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- heteroaryl
- aryl
- cycloalkyl
- aralkyl
- Prior art date
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Classifications
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- 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
- A61K31/407—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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente se refiere a métodos para usar compuestos de espiro-oxindol de la formula (1): en donde k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, y R3d son como se definen en la presente, como uno de sus estereoisomeros, enantiomeros, tautomeros o mezclas de ellos; o una de sus sales, solvatos o prodrogas farmacéuticamente aceptables, para el tratamiento y/o la prevencion de hipercolesterolemia, hiperplasia benigna de prostata, pruritis y cáncer. Reivindicacion 1: Un método para el tratamiento o la prevencion de hipercolesterolemia en un mamífero, caracterizado porque comprende la administracion al mamífero que lo necesita una cantidad terapéuticamente efectiva de un compuesto de formula (1), donde: j y k son cada uno en forma independiente 0, 1, 2 o 3; Q es -C(R1a)H-, -C(O)-, -O-, -S(O)m- (donde m es 0, 1 o 2), -CF2-, -C(O)O-, -C(O)N(R5)- o - N(R5)C(O)-; R1a es hidrogeno u -OR5; R1 es hidrogeno, alquilo, alquenilo, alquinilo, haloalquilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heterociclilo, -R8-C(O)R5, -R8-C(O)OR5, -R8-C(O)N(R4)R5, -S(O)2-R5, -R9-S(O)m-R5 (donde m es 0, 1 o 2), -R8-OR5, -R8-CN, -R9-P(O)(OR5)2, o -R9-O-R9-OR5; o R1 es aralquilo sustituido con -C(O)N(R6)R7 donde: R6 es hidrogeno, alquilo, arilo o aralquilo; y R7 es hidrogeno, alquilo, haloalquilo, -R9-CN, -R9-OR5, -R9-N(R4)R5, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo; o R6 y R7, junto con el nitrogeno al cual se encuentran unidos, forman un heterociclilo o heteroarilo; y en donde cada grupo arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilo para R6 y R7 puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en alquilo, cicloalquilo, arilo, aralquilo, halo, haloalquilo, -R8-CN, -R8-OR5, heterociclilo y heteroarilo; o R1 es aralquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en -R8-OR5, -C(O)OR5, halo, haloalquilo, alquilo, nitro, ciano, arilo, aralquilo, heterociclilo y heteroarilo; o R1 es -R9-N(R10)R11, -R9-N(R12)C(O)R11 o -R9-N(R10)C(O)N(R10)R11 donde cada R10 es H, alquilo, arilo, aralquilo o heteroarilo; cada R11 es hidrogeno, alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo, -R9-OC(O)R5, -R9- C(O)OR5, -R9-C(O)N(R4)R5, -R9-C(O)R5, -R9-N(R4)R5, -R9-OR5, o -R9-CN; R12 es hidrogeno, alquilo, arilo, aralquilo o -C(O)R5; y donde cada grupo arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo para R10 y R11 puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste de alquilo, cicloalquilo, arilo, aralquilo, halo, haloalquilo, nitro, -R8-CN, -R8-OR5, -R8-C(O)R5, heterociclilo y heteroarilo; o R1 es heterociclilalquilo o heteroarilalquilo donde el grupo heterociclilalquilo o heteroarilalquilo está opcionalmente sustituido por uno o más sustituyentes seleccionados entre el grupo que consiste en oxo, alquilo, halo, haloalquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo, -R8-OR5, -R8-C(O)OR5, -R8-N(R4)R5, -R8-C(O)N(R4)R5, -R8-N(R5)C(O)R4, -R8-S(O)mR4 (donde m es 0, 1 o 2), -R8- CN, o -R8-NO2; R2a, R2b, R2c y R2d se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrogeno, alquilo, alquenilo, alquinilo, alcoxi, halo, haloalquilo, haloalquenilo, haloalcoxi, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, aralquenilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo, -R8-CN, -R8-NO2, -R8-OR5, -R8-N(R4)R5, -N=C(R4)R5, S(O)mR4, -OS(O)2CF3, -R8-C(O)R4, -C(S)R4, -C(R4)2C(O)R5, -R8-C(O)OR4, -C(S)OR4, -R8-C(O)N(R4)R5, - C(S)N(R4)R5, -N(R5)C(O)R4, -N(R5)C(S)R4, -N(R5)C(O)OR4, -N(R5)C(S)OR4, -N(R5)C(O)N(R4)R5, -N(R5)C(S)N(R4)R5, -N(R5)S(O)nR4, -N(R5)S(O)n(R4)R5, -R8-S(O)nN(R4)R5, -N(R5)C(=NR5)N(R4)R5, y -N(R5)C(=N-CN)N(R4)R5, en donde cada m es en forma independiente 0, 1, o 2 y cada n es en forma independiente 1 o 2; y donde cada uno de los grupos cicloalquilo, cicloalquilalquilo, arilo, aralquilo, aralquenilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo para R2a, R2b, R2c y R2d puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en alquilo, alquenilo, alquinilo, alcoxi, halo, haloalquilo, haloalquenilo, haloalcoxi, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, aralquenilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo, -R8-CN, -R8-NO2, -R8-OR5, -R8-N(R4)R5, -S(O)mR4, -R8-S(O)nN(R4)R5, -R8-C(O)R4, -R8-C(O)OR4, -R8-C(O)N(R4)R5, -N(R5)C(O)R4, y -N(R5)S(O)nR4, donde cada m es en forma independiente 0, 1, o 2 y cada n es en forma independiente 1 o 2; o R2a y R2b, junto con los átomos de carbono del anillo a los que están directamente unidos, pueden formar un anillo fusionado seleccionado entre cicloalquilo, arilo, heterociclilo y heteroarilo, y R2c y R2d son como se ha definido; o R2b y R2c, junto con los átomos de carbono del anillo a los que están directamente unidos, pueden formar un anillo fusionado seleccionado entre cicloalquilo, arilo, heterociclilo y heteroarilo, y R2a y R2d son como se ha definido; o R2c y R2d, junto con los átomos de carbono del anillo a los que están directamente unidos, pueden formar un anillo fusionado seleccionado entre cicloalquilo, arilo, heterociclilo y heteroarilo, y R2a y R2b son como se ha definido; R3a, R3b, R3c y R3d se seleccionan en forma independiente entre sí entre el grupo que consiste de hidrogeno, alquilo, alquenilo, alquinilo, alcoxi, halo, haloalquilo, haloalquenilo, haloalcoxi, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, aralquenilo, heterociclilo, heterociclilalquilo, heteroarilo, heteroarilalquilo, -R8-CN, -R8-NO2, -R8-OR5, -R8-N(R4)R5, -N=C(R4)R5, - S(O)mR4, -OS(O)2CF3, -R8-C(O)R4, -C(S)R4, -C(R4)2C(O)R5, R8-C(O)OR4, -C(S)OR4, -R8-C(O)N(R4)R5, - C(S)N(R4)R5, -N(R5)C(O)R4, -N(R5)C(S)R4, -N(R5)C(O)OR4, -N(R5)C(S)OR4, -N(R5)C(O)N(R4)R5, -N(R5)C(S)N(R4)R5, -N(R5)S(O)nR4, -N(R5)S(O)nN(R4)R5, -R8-S(O)nN(R4)R5, -N(R5)C(=NR5)N(R4)R5, y -N(R5)C(N=C(R4)R5)N(R4)R5, donde cada m es en forma independiente 0, 1, o 2 y cada n es en forma independiente 1 o 2; o R3a y R3b, junto con los átomos de carbono del anillo a los que están directamente unidos, forman un anillo fusionado seleccionado entre cicloalquilo, heterociclilo, arilo o heteroarilo, y R3c y R3d son como se ha definido; o R3b y R3c, junto con los átomos de C del anillo a los que están directamente unidos, pueden formar un anillo fusionado seleccionado entre cicloalquilo, heterociclilo, arilo o heteroarilo, y R3a y R3d son como se ha definido; o R3c y R3d junto con los átomos de C del anillo a los que están directamente unidos, pueden formar un anillo fusionado seleccionado entre cicloalquilo, heterociclilo, arilo o heteroarilo, y R3a y R3b son como se ha definido; cada R4 y R5 se selecciona en forma independiente entre grupo que consiste de hidrogeno, alquilo, alquenilo, alquinilo, haloalquilo, alcoxialquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo, y heteroarilalquilo; o cuando R4 y R5 están ambos unidos al mismo átomo de nitrogeno, entonces R4 y R5, junto con el átomo de nitrogeno al cual están unidos, pueden formar un heterociclilo o heteroarilo; y cada R8 en un enlace directo o una cadena alquileno lineal o ramificada, una cadena alquenileno lineal o ramificada o una cadena alquinileno lineal o ramificada; y cada R9 es una cadena alquileno lineal o ramificada, una cadena alquenileno lineal o ramificada o una cadena alquinileno lineal o ramificada; como estereoisomeros, enantiomeros, tautomeros del mismo o mezclas de los mismos; o solvatos, prodrogas o sales aceptable para uso farmacéutico del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US85178706P | 2006-10-12 | 2006-10-12 |
Publications (1)
Publication Number | Publication Date |
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AR063280A1 true AR063280A1 (es) | 2009-01-21 |
Family
ID=39339863
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070104540A AR063280A1 (es) | 2006-10-12 | 2007-10-12 | Uso de compuestos de espiro-oxindol como agentes terapeuticos |
Country Status (14)
Country | Link |
---|---|
US (1) | US8466188B2 (es) |
EP (1) | EP2073806B1 (es) |
JP (2) | JP5460324B2 (es) |
CN (2) | CN103271906A (es) |
AR (1) | AR063280A1 (es) |
AT (1) | ATE545416T1 (es) |
AU (1) | AU2007319580B2 (es) |
BR (1) | BRPI0719210A2 (es) |
CA (1) | CA2665698A1 (es) |
CL (1) | CL2007002950A1 (es) |
MX (1) | MX2009003876A (es) |
RU (1) | RU2009117642A (es) |
TW (1) | TW200833695A (es) |
WO (1) | WO2008060789A2 (es) |
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US8263606B2 (en) * | 2008-10-17 | 2012-09-11 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
EP2350091B1 (en) | 2008-10-17 | 2015-06-03 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
WO2010053998A1 (en) | 2008-11-05 | 2010-05-14 | Xenon Pharmaceuticals, Inc. | Spiro-condensed indole derivatives as sodium channel inhibitors |
US20110269788A1 (en) * | 2008-12-29 | 2011-11-03 | Xenon Pharmaceuticals Inc. | Spiro-oxindole-derivatives as sodium channel blockers |
WO2010132352A2 (en) | 2009-05-11 | 2010-11-18 | Xenon Pharmaceuticals Inc. | Spiro compounds and their use as therapeutic agents |
AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
EP2733145A1 (en) | 2009-10-14 | 2014-05-21 | Xenon Pharmaceuticals Inc. | Synthetic methods for spiro-oxindole compounds |
WO2011047173A2 (en) | 2009-10-14 | 2011-04-21 | Xenon Pharmaceuticals Inc. | Pharmaceutical compositions for oral administration |
PE20121699A1 (es) | 2010-02-26 | 2012-12-22 | Xenon Pharmaceuticals Inc | Composiciones farmaceuticas del compuesto espiro-oxindol para administracion topica |
-
2007
- 2007-10-12 CL CL200702950A patent/CL2007002950A1/es unknown
- 2007-10-12 RU RU2009117642/15A patent/RU2009117642A/ru not_active Application Discontinuation
- 2007-10-12 AT AT07868434T patent/ATE545416T1/de active
- 2007-10-12 MX MX2009003876A patent/MX2009003876A/es active IP Right Grant
- 2007-10-12 AU AU2007319580A patent/AU2007319580B2/en not_active Ceased
- 2007-10-12 CA CA002665698A patent/CA2665698A1/en not_active Abandoned
- 2007-10-12 BR BRPI0719210 patent/BRPI0719210A2/pt not_active IP Right Cessation
- 2007-10-12 CN CN2013101646702A patent/CN103271906A/zh active Pending
- 2007-10-12 EP EP07868434A patent/EP2073806B1/en not_active Not-in-force
- 2007-10-12 TW TW096138356A patent/TW200833695A/zh unknown
- 2007-10-12 JP JP2009532606A patent/JP5460324B2/ja not_active Expired - Fee Related
- 2007-10-12 WO PCT/US2007/081247 patent/WO2008060789A2/en active Application Filing
- 2007-10-12 AR ARP070104540A patent/AR063280A1/es unknown
- 2007-10-12 US US12/445,264 patent/US8466188B2/en active Active
- 2007-10-12 CN CN200780038111A patent/CN101631546A/zh active Pending
-
2013
- 2013-09-30 JP JP2013204440A patent/JP2013256539A/ja not_active Withdrawn
Also Published As
Publication number | Publication date |
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US8466188B2 (en) | 2013-06-18 |
EP2073806B1 (en) | 2012-02-15 |
MX2009003876A (es) | 2009-05-11 |
TW200833695A (en) | 2008-08-16 |
ATE545416T1 (de) | 2012-03-15 |
CN101631546A (zh) | 2010-01-20 |
AU2007319580B2 (en) | 2012-11-29 |
BRPI0719210A2 (pt) | 2015-05-05 |
JP2013256539A (ja) | 2013-12-26 |
CN103271906A (zh) | 2013-09-04 |
WO2008060789A3 (en) | 2008-07-24 |
US20100173967A1 (en) | 2010-07-08 |
US20110172282A9 (en) | 2011-07-14 |
RU2009117642A (ru) | 2010-11-20 |
JP2010506854A (ja) | 2010-03-04 |
CA2665698A1 (en) | 2008-05-22 |
AU2007319580A1 (en) | 2008-05-22 |
JP5460324B2 (ja) | 2014-04-02 |
EP2073806A2 (en) | 2009-07-01 |
CL2007002950A1 (es) | 2008-02-01 |
WO2008060789A2 (en) | 2008-05-22 |
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