AR042691A1 - Agonistas inversos del receptor cb1 procedimientos de obtencion y composiciones farmaceuticas. - Google Patents
Agonistas inversos del receptor cb1 procedimientos de obtencion y composiciones farmaceuticas.Info
- Publication number
- AR042691A1 AR042691A1 ARP030104878A ARP030104878A AR042691A1 AR 042691 A1 AR042691 A1 AR 042691A1 AR P030104878 A ARP030104878 A AR P030104878A AR P030104878 A ARP030104878 A AR P030104878A AR 042691 A1 AR042691 A1 AR 042691A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- substituted
- lower alkoxy
- tri
- hydroxyl
- Prior art date
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P25/06—Antimigraine agents
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P25/16—Anti-Parkinson drugs
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- Diabetes (AREA)
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- Endocrinology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
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- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
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Abstract
Los compuestos son útiles para el tratamiento y/o prevención de enfermedades que están asociadas con la modulación de los receptores CB1. Reivindicación 1: Compuestos de fórmula (1), en donde: X es C ó N; R2 es alquilo inferior o -(CH2)n-R2a; R2a es cicloalquilo, opcionalmente mono-, di-, tri- o tetra-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, alquilo inferior fluorado o alcoxilo inferior fluorado; un anillo heterocíclico saturado monovalente de 5 ó 6 miembros que contiene de uno a tres heteroátomos independientemente seleccionado de nitrógeno, oxígeno y azufre, estando dicho anillo heterocíclico opcionalmente mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, amino, alquilamino inferior, cicloalquilo, oxo, alquilo inferior fluorado o alcoxilo inferior fluorado; un anillo heteroaromático de 5 ó 6 miembros monovalente que contiene de una a cuatro heteroátomos independientemente seleccionados de nitrógeno, oxígeno y azufre, estando dicho anillo heteroaromático opcionalmente mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, amino, alquilamino inferior o cicloalquilo; o fenilo, que puede estar opcionalmente mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, alquilamino inferior, alquilo inferior halogenado, alcoxilo inferior halogenado o nitro; R3 es cicloalquilo, opcionalmente mono-, di- o tri o tetra-sustituido, alcoxilo inferior, alquilo inferior fluorado o alcoxilo inferior fluorado; o fenilo, que puede estar opcionalmente mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, alquilamino inferior, alquilo inferior halogenado, alcoxilo inferior halogenado o nitro; R4 es un anillo heteroaromático monovalente de 5 ó 6 miembros que contiene de uno a tres heteroátomos independientemente seleccionados de nitrógeno, oxígeno y azufre, estando dicho anillo heteroaromático opcionalmente mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, amino, alquilamino inferior; naftilo, que puede opcionalmente estar mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, alquilamino inferior, alquilo inferior halogenado, alcoxilo inferior halogenado o nitro; o fenilo que puede opcionalmente estar mono-, di- o tri-sustituido, independientemente, por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, nitro, alquilo inferior halogenado, alcoxilo inferior halogenado, ciano, alquilsulfonilo inferior o -NR7R8; o dos sustituyentes adyacentes de dicho residuo fenilo juntos son -O-(CH2)p-O- o -(CH2)2-C(O)NH-; R5 y R6 son cada uno independientemente hidrógeno, alquilo inferior, halógeno o metilo fluorado; R7 y R8 son cada uno independientemente hidrógeno o alquilo inferior; o R7 y R8 junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico aromático o saturado de 5 ó 6 miembros que opcionalmente contiene otro o otros dos heteroátomos independientemente seleccionados de nitrógeno, oxígeno y azufre, estando dicho anillo heterocíclico aromático o saturado opcionalmente sustituido por hidroxilo, alquilo inferior, alcoxilo inferior, halógeno, amino o alquilamino inferior; m es 0, 1 ó 2; n es 0 ó 1; p es 1, 2 ó 3; y sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03000003 | 2003-01-02 |
Publications (1)
Publication Number | Publication Date |
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AR042691A1 true AR042691A1 (es) | 2005-06-29 |
Family
ID=32695582
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030104878A AR042691A1 (es) | 2003-01-02 | 2003-12-30 | Agonistas inversos del receptor cb1 procedimientos de obtencion y composiciones farmaceuticas. |
Country Status (18)
Country | Link |
---|---|
US (2) | US7294644B2 (es) |
EP (1) | EP1583742B1 (es) |
JP (1) | JP4444120B2 (es) |
KR (1) | KR100704097B1 (es) |
CN (2) | CN101012193A (es) |
AR (1) | AR042691A1 (es) |
AT (1) | ATE450505T1 (es) |
AU (1) | AU2003298227A1 (es) |
BR (1) | BR0317926A (es) |
CA (1) | CA2511859A1 (es) |
CL (1) | CL2003002770A1 (es) |
DE (1) | DE60330392D1 (es) |
ES (1) | ES2334565T3 (es) |
MX (1) | MXPA05007114A (es) |
PL (1) | PL378206A1 (es) |
RU (1) | RU2339618C2 (es) |
TW (1) | TW200413328A (es) |
WO (1) | WO2004060870A1 (es) |
Families Citing this family (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2003007887A2 (en) | 2001-07-20 | 2003-01-30 | Merck & Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
ATE486842T1 (de) | 2002-03-12 | 2010-11-15 | Merck Sharp & Dohme | Substituierte amide |
FR2845382A1 (fr) * | 2002-10-02 | 2004-04-09 | Sanofi Synthelabo | Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique |
ES2309383T3 (es) * | 2003-01-02 | 2008-12-16 | Hoffmann La Roche | Pirrolil tiazoles y su empleo como agonistas inversos de receptores cb1. |
JP2007509104A (ja) * | 2003-10-24 | 2007-04-12 | グラクソ グループ リミテッド | 複素環式化合物 |
GB0403780D0 (en) * | 2004-02-20 | 2004-03-24 | Astrazeneca Ab | Therapeutic agents |
EP1568698A1 (en) * | 2004-02-27 | 2005-08-31 | Aventis Pharma Deutschland GmbH | Pyrrole-derivatives as factor Xa inhibitors |
RU2377238C2 (ru) | 2004-04-03 | 2009-12-27 | Астразенека Аб | Производные имидазола, активные в отношении рецептора св1 |
US8026237B2 (en) * | 2004-07-30 | 2011-09-27 | Exelixis, Inc. | Pyrrole derivatives as pharmaceutical agents |
FR2874012B1 (fr) * | 2004-08-09 | 2008-08-22 | Sanofi Synthelabo | Derives de pyrrole, leur preparation et leur utlisation en therapeutique |
CN102633730A (zh) | 2004-12-03 | 2012-08-15 | 先灵公司 | 作为cb1拮抗剂的取代哌嗪 |
EP2368881A1 (en) * | 2005-01-10 | 2011-09-28 | University of Connecticut | Heteropyrazole analogs acting on cannabinoid receptors |
AU2006264649A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | GPCR agonists |
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-
2003
- 2003-12-22 WO PCT/EP2003/014720 patent/WO2004060870A1/en active Application Filing
- 2003-12-22 PL PL378206A patent/PL378206A1/pl not_active Application Discontinuation
- 2003-12-22 RU RU2005124360/04A patent/RU2339618C2/ru not_active IP Right Cessation
- 2003-12-22 KR KR1020057012530A patent/KR100704097B1/ko not_active IP Right Cessation
- 2003-12-22 EP EP03795949A patent/EP1583742B1/en not_active Expired - Lifetime
- 2003-12-22 CN CNA200710085476XA patent/CN101012193A/zh active Pending
- 2003-12-22 TW TW092136400A patent/TW200413328A/zh unknown
- 2003-12-22 MX MXPA05007114A patent/MXPA05007114A/es active IP Right Grant
- 2003-12-22 BR BR0317926-5A patent/BR0317926A/pt not_active IP Right Cessation
- 2003-12-22 CA CA002511859A patent/CA2511859A1/en not_active Abandoned
- 2003-12-22 AT AT03795949T patent/ATE450505T1/de not_active IP Right Cessation
- 2003-12-22 CN CNB2003801082687A patent/CN100395234C/zh not_active Expired - Fee Related
- 2003-12-22 AU AU2003298227A patent/AU2003298227A1/en not_active Abandoned
- 2003-12-22 ES ES03795949T patent/ES2334565T3/es not_active Expired - Lifetime
- 2003-12-22 JP JP2004564210A patent/JP4444120B2/ja not_active Expired - Fee Related
- 2003-12-22 US US10/743,642 patent/US7294644B2/en not_active Expired - Fee Related
- 2003-12-22 DE DE60330392T patent/DE60330392D1/de not_active Expired - Lifetime
- 2003-12-29 CL CL200302770A patent/CL2003002770A1/es unknown
- 2003-12-30 AR ARP030104878A patent/AR042691A1/es unknown
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2007
- 2007-05-10 US US11/801,727 patent/US7579369B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
PL378206A1 (pl) | 2006-03-20 |
MXPA05007114A (es) | 2005-08-26 |
CL2003002770A1 (es) | 2005-01-07 |
US20040167129A1 (en) | 2004-08-26 |
US7579369B2 (en) | 2009-08-25 |
US20070238754A1 (en) | 2007-10-11 |
CN1735593A (zh) | 2006-02-15 |
EP1583742B1 (en) | 2009-12-02 |
BR0317926A (pt) | 2005-11-29 |
TW200413328A (en) | 2004-08-01 |
RU2339618C2 (ru) | 2008-11-27 |
WO2004060870A1 (en) | 2004-07-22 |
DE60330392D1 (de) | 2010-01-14 |
KR20050091055A (ko) | 2005-09-14 |
CN101012193A (zh) | 2007-08-08 |
CN100395234C (zh) | 2008-06-18 |
JP4444120B2 (ja) | 2010-03-31 |
EP1583742A1 (en) | 2005-10-12 |
JP2006521281A (ja) | 2006-09-21 |
KR100704097B1 (ko) | 2007-04-06 |
RU2005124360A (ru) | 2006-06-10 |
ATE450505T1 (de) | 2009-12-15 |
CA2511859A1 (en) | 2004-07-22 |
AU2003298227A1 (en) | 2004-07-29 |
US7294644B2 (en) | 2007-11-13 |
ES2334565T3 (es) | 2010-03-12 |
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