AR057357A1 - Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticas - Google Patents
Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticasInfo
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- AR057357A1 AR057357A1 ARP060102405A ARP060102405A AR057357A1 AR 057357 A1 AR057357 A1 AR 057357A1 AR P060102405 A ARP060102405 A AR P060102405A AR P060102405 A ARP060102405 A AR P060102405A AR 057357 A1 AR057357 A1 AR 057357A1
- Authority
- AR
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- Prior art keywords
- heteroaryl
- heterocyclyl
- aryl
- alkyl
- optionally substituted
- Prior art date
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- 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
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- 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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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P27/00—Drugs for disorders of the senses
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- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- 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
- A61P9/12—Antihypertensives
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Abstract
Reivindicacion 1: Compuesto caracterizado porque la formula W-L-Z enantiomeros, diastereomeros, solvatos, sales o profármacos del mismo, en donde: W es arilo, cicloalquilo, heteroarilo o heterociclilo, todos los cuales pueden ser opcionalmente sustituidos con R1, R1a, R1b, R1c y R1d; R1, R1a, R1b, R1c y R1d son independientemente hidrogeno, halogeno, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, SOR2a, SO2R2a, -NR2SO2R6, -NR2CO2R6, alquilo, haloalquilo, cicloalquilo, alcoxi, ariloxi, alquenilo, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, aminoalquilo, arilamino, heteroarilamino, arilo, heteroarilo o heterociclilo, en donde el arilo, heteroarilo o heterociclilo pueden ser opcionalmente sustituidos con R7, R7a, R7b y R7c; o alternativamente algunos dos de R1, R1a, R1b, R1c y R1d se pueden tomar conjuntamente para formar un anillo de arilo, heteroarilo, heterociclilo fusionado o anillo heterociclilo espiro; L es un enlace, O, S, SO, SO2, alquenilo, cicloalquilo, NR5, CR2R2a, CR2CR2aCR2bR2c, SO2NR2, OCR2R2a, OCR2R2aCR2bR2c, CR2R2aO, CR2bR2cCR2R2aO, N(R5)CR2R2a, CR2R2aN(R5), SCR2R2a, CR2R2aS, CR2R2aSO, CR2R2aSO2, SOCR2R2a, SO2CR2R2a, CR2R2aOCR2bR2c, CR2R2aSCR2bR2c, CR2R2SO2CR2bR2c, SO2NR2CR2aR2b, COCR2R2a. CR2R2aCO, CONR5CR2aR2b, CR2R2aCR2bR2cS, CR2R2aCR2bR2cSO, siempre que L no sea un enlace cuendo W es fenilo; R2, R2a, R2b y R2c son independientemente hidrogeno, halogeno, alquilo o halo alquilo; o alternativamente algunos dos de R2, R2a, R2b y R2c se pueden tomar conjuntamente con el átomo al cual se unen para formar un anillo cicloalquilo, cicloalquilo sustituido con halogeno o heterociclilo; Z se selecciona de los siguientes grupos heteroarilo bicíclicos: (a) (b) (c) (d) (e) (f) (g) (h); R3, R3a y R3b son independientemente hidrogeno, halogeno, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alquilo, haloalquilo, cicloalquilo, alcoxi, ariloxi, alquenilo, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, aminoalquilo, arilamino, heteroatilamino, arilo, heteroarilo o heterociclilo, en donde el arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b y R7c, R4 es bibiclo[2,2,2]octilo o biciclo[2,2,1]heptilo, ambos se pueden sustituir opcionalmente con uno o más sustituyentes seleccionados de halogeno, -OH, OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, CONR2R2a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b y R7c; o R4 cicloalquilo, diferente de biciclo[2,2,2]octilo o biciclo[2,2,1]heptilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4 es heterociclilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, OCONR2R2a, -NR5CO2R6, SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4 es alquilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, OR6, -SR6, -OCOR6, -CN, -NR5COR6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4a es hidrogeno, CN, alquilo, haloalquilo, arilo, arilosustituido, heteroarilo o heteroarilo sustituido; R5 en cada caso, es independientemente hidrogeno, alquilo, cicloalquilo, arilo, haloalquilo, COR2a, CO2R2a, SO2NR2R2a, o SO2R2a; R6, en cada caso, es independientemente alquilo, cicloalquilo, arilo o heteroarilo, todos los cuales se pueden sustituir opcionalmente con R7, R7a, R7b, y R7c; y R7, R7a, R7b, y R7b, en cada caso, son independientemente halo, alquilo, haloalquilo, alcoxi, arilo, ariloxi, arilarilo, arilalquilo, arilalquiloxi, alquenilo, cicloalquilo , cicloalquilalquilo, cicloalquilalquiloxi, amino, -OH, hidroxialquilo, acilo, heteroarilo, heteroariloxi, heteroarilalquilo, heteroarilalcoxi, ariloxialquilo, alquiltio, arilalquiltio, ariloxiarilo, alquilamido, alcanoilamino, arilcarbonilamino, - NO2, -CN o tiol; excluyendo los compuestos que tienen la formula (1) en donde W es fenilo, el fenilo es opcionalmente sustituido con R1, R1a, R1b, R1c y R1d; R1, R1a, R1b, R1c y R1d son independientemente hidrogeno, halogeno, alquilo o haloalquilo; Les CH2, O, S o SO2; y R4 es C3-10cicloalquilo, diferente de biciclo[2,2,2]octilo o biciclo [2,2,1]heptilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, -NHCOR6, -NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo; o R4 es C1-10heterociclilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, -NHCOR6, - NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo; o R4 es C1-6alquilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, - NHCOR6, -NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo. Composiciones farmacéuticas que los comprenden.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US68899305P | 2005-06-09 | 2005-06-09 | |
US11/448,946 US7572807B2 (en) | 2005-06-09 | 2006-06-07 | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
Publications (1)
Publication Number | Publication Date |
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AR057357A1 true AR057357A1 (es) | 2007-11-28 |
Family
ID=37524860
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060102405A AR057357A1 (es) | 2005-06-09 | 2006-06-08 | Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticas |
Country Status (12)
Country | Link |
---|---|
US (2) | US7572807B2 (es) |
EP (1) | EP1912986B1 (es) |
JP (1) | JP5124450B2 (es) |
KR (1) | KR20080018942A (es) |
AR (1) | AR057357A1 (es) |
AU (1) | AU2006258077B2 (es) |
ES (1) | ES2392656T3 (es) |
MX (1) | MX2007015283A (es) |
NO (1) | NO20076054L (es) |
PE (1) | PE20070002A1 (es) |
TW (1) | TW200716116A (es) |
WO (1) | WO2006135667A1 (es) |
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GB0420722D0 (en) * | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
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TWI417095B (zh) | 2006-03-15 | 2013-12-01 | Janssen Pharmaceuticals Inc | 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途 |
WO2007121578A1 (en) * | 2006-04-24 | 2007-11-01 | Merck Frosst Canada Ltd. | Indole amide derivatives as ep4 receptor antagonists |
PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
PE20121506A1 (es) | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
EP2070927A4 (en) * | 2006-09-13 | 2010-10-13 | Kyowa Hakko Kirin Co Ltd | CONDENSED HETEROCYCLIC DERIVATIVE |
CA2665195C (en) * | 2006-10-11 | 2011-08-09 | Amgen Inc. | Imidazo- and triazolo-pyridine compounds and methods of use thereof |
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CN101679409B (zh) | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
CA2672172C (en) | 2006-12-22 | 2016-05-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
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TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
WO2008130951A1 (en) | 2007-04-17 | 2008-10-30 | Bristol-Myers Squibb Company | Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors |
EP2170337A4 (en) * | 2007-06-28 | 2013-12-18 | Abbvie Inc | NEW TRIAZOLOPYRIDAZINE |
US20090069288A1 (en) * | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
JP5366269B2 (ja) | 2007-09-14 | 2013-12-11 | ジャンセン ファーマシューティカルズ, インコーポレイテッド. | 1,3−二置換4−(アリル−x−フェニル)−1h−ピリジン−2−オン |
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GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
US8785486B2 (en) | 2007-11-14 | 2014-07-22 | Janssen Pharmaceuticals, Inc. | Imidazo[1,2-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
EP2072516A1 (en) * | 2007-12-21 | 2009-06-24 | Santhera Pharmaceuticals (Schweiz) AG | Substituted imidazopyridine derivates as Melancortin-4 receptor antagonists |
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- 2006-06-08 EP EP06772525A patent/EP1912986B1/en active Active
- 2006-06-08 PE PE2006000635A patent/PE20070002A1/es not_active Application Discontinuation
- 2006-06-08 AR ARP060102405A patent/AR057357A1/es unknown
- 2006-06-08 WO PCT/US2006/022260 patent/WO2006135667A1/en active Application Filing
- 2006-06-08 JP JP2008515911A patent/JP5124450B2/ja not_active Expired - Fee Related
- 2006-06-08 KR KR1020087000470A patent/KR20080018942A/ko not_active Application Discontinuation
-
2007
- 2007-11-26 NO NO20076054A patent/NO20076054L/no not_active Application Discontinuation
-
2009
- 2009-07-27 US US12/509,541 patent/US8158648B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
JP5124450B2 (ja) | 2013-01-23 |
TW200716116A (en) | 2007-05-01 |
EP1912986A1 (en) | 2008-04-23 |
US8158648B2 (en) | 2012-04-17 |
EP1912986B1 (en) | 2012-09-05 |
AU2006258077A1 (en) | 2006-12-21 |
WO2006135667A1 (en) | 2006-12-21 |
JP2008543764A (ja) | 2008-12-04 |
KR20080018942A (ko) | 2008-02-28 |
US7572807B2 (en) | 2009-08-11 |
US20060281750A1 (en) | 2006-12-14 |
NO20076054L (no) | 2008-03-04 |
ES2392656T3 (es) | 2012-12-12 |
MX2007015283A (es) | 2008-02-25 |
PE20070002A1 (es) | 2007-01-18 |
US20090306084A1 (en) | 2009-12-10 |
AU2006258077B2 (en) | 2012-02-23 |
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