AR039842A1 - Compuestos heterociclicos sustituidos y metodos de empleo - Google Patents

Compuestos heterociclicos sustituidos y metodos de empleo

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Publication number
AR039842A1
AR039842A1 ARP030101777A ARP030101777A AR039842A1 AR 039842 A1 AR039842 A1 AR 039842A1 AR P030101777 A ARP030101777 A AR P030101777A AR P030101777 A ARP030101777 A AR P030101777A AR 039842 A1 AR039842 A1 AR 039842A1
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Argentina
Prior art keywords
alkyl
substituted
independently
instance
nrgrg
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ARP030101777A
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English (en)
Inventor
Celia Dominguez
Henry Q Zhang
Guo-Qiang Cao
Martin H Goldberg
Fang-Tsao Hong
Kelvin K C Sham
Seifu Tadesse
Nuria A Tamayo
Kurt E Weiler
Hongyu Liao
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Amgen Inc
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Publication of AR039842A1 publication Critical patent/AR039842A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptable, donde: n es 0, 1 ó 2; R1 es una cadena cerrada de 5, 6 ó 7 miembros, saturada o insaturada, que contiene 0, 1, 2 ó 3 átomos seleccionados de N, O y S, donde la cadena cerrada puede estar fusionada con un grupo benzo, y está sustituida por 0, 1 ó 2 grupos oxo, y donde R1 está adicionalmente sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd y alquilo C1-4Rd; R2 es alquilo C1-6 sustituido con 1, 2 ó 3 grupos Rd y 0 ó 1 grupos Rc, que están sustituidos por 0, 1 ó 2 grupos Rd, donde R2 no es -C(=O)Obencilo; y donde -R1-R2 no es 3-bencilpiperazin-1-ilo; y donde si tanto R3 como R4 son 4-metilfenilo, -R1-R2 no es 4-(hidroximetil)piperidin-1-ilo; R3 es Rc sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rf y Rd; R4 es Rc sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rf y Rd que no incluyen 1-feniletilamino; siempre que el número total de grupos Rc sustituidos en cada uno de R3 y R4 sea 0 ó 1; R5 es independientemente en cada instancia H, alquilo C1-8 o alquilo C1-6Rc, ambos sustituidos por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd; R6 es independientemente en cada instancia alquilo C1-8 o alquilo C1-6Rc, ambos sustituidos por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd; o R6 es Rd; R7 es independientemente hidrógeno, -alquilo C1-6 o -alquilo C1-4Rc, donde cualquier átomo de carbono de la estructura anterior está sustituido por 0 a 3 sustituyentes seleccionados de Rd; Ra es independientemente en cada instancia h O Rb; Rb es independientemente en cada instancia alquilo C1-8, Rc o alquilo C1-4Rc, cada uno de los cuales está sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados independientemente de Rd; Rc es independientemente en cada instancia arilo o una cadena cerrada heterocíclica de 5, 6 ó 7 miembros saturado o insaturada, que contiene 1, 2 ó 3 átomos seleccionados de N, O y S, donde la cadena cerrada está fusionada con 0 ó 1 grupos benzo y 0 ó 1 cadenas cerradas heterocíclicas de 5, 6 ó 7 miembros, saturadas o insaturadas, que contienen 1, 2 ó 3 átomos seleccionados de N, O y S; donde cualquier cadena cerrada heterocíclica está sustituida por 0, 1 ó 2 grupos oxo; Rd es independientemente en cada instancia alquilo C1-6, halo, haloalquilo C1-4, ciano, -C(=O)Rf, -C(=O)ORe, -C(=O)NRgRg, -C(=NRg)NRgRg, -ORe, --OC(=O)Re, -OC(=O)NRgRg, -OC(=O)N(Rh)S(=O)2Rf, -SRe, -S(=O)Rf, -S(=O)2Rf, -S(=O)2NRgRg, -S(=O)2N(Rh)C(=O)Rf, -S(=O)2N(Rh)C(=O)ORf, -S(=O)2-N(Rh)C(=O)NRgRg, -NRgRg, -N(Rh)C(=O)Re, -N(Rh)C(=O)ORf, -N(Rh)C(=O)NRgRg, -N(Rh)C(=NRg)NRgRg, -N(Rh)S(=O)2Rf ó -N(Rh)S(=O)NRgRg; Re es independientemente en cada instancia hidrógeno o Rf; Rf es independientemente en cada instancia Rc o alquilo C1-8, cualquiera de los cuales está sustituido por 0 a 3 sustituyentes seleccionados de -NRgRg, -C(=O)ORi, -ORi,-N(Ri)C(=O)Rk, -N(Ri)C(=O)ORi, -N(Ri)S(=O)2Rk, -S(=O)nRk, ciano, halo, -O alquilo C1-4 Rc, -S(=O)n alquilo C1-4 Rc y Rc, donde cualquier Rc en Rf puede estar sustituido, también, por alquilo C1-8 o haloalquilo C1-4; Rg es independientemente en cada instancia hidrógeno, Rc, alquilo C1-10 o -alquilo C1-4Rc, donde cada uno está sustituido por 0 a 3 sustituyentes seleccionados de -NRiRi, -N(Ri)C(=O)Rk, -N(Ri)C(=O)ORk, -N(Ri)S(=O)2Rk, -ORi, -S(=O)nRk, ciano, alquilo C1-8 y haloalquilo C1-4; Rh independientemente en cada instancia hidrógeno, alquilo C1-8 o alquilo C1-4Rc cada uno de los cuales está sustituido por 0 a 3 sustituyentes seleccionados de -NRiRi, -N(Ri)C(=O)Rk, -N(Ri)C(=O)ORk, -N(Ri)S(=O)2Rk, -ORi, -S(=O)nRk, ciano, alquilo C1-8 y haloalquilo C1-4; Ri es Rk o hidrógeno; Rk es alquilo C1-6, fenilo o bencilo; V es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; W es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; y X es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; donde el número total de grupos -NR5-, C=O, C=S o C=NR7 representados por V, W y X debe ser 0 ó 2; y al menos uno de V, W y X contiene un átomo de N. También se incluye un método para la profilaxis o el tratamiento de: inflamación, artritis reumatoidea, mal de Paget, osteoporosis, mieloma múltiple, uveitis, leucemia mielógeno aguda o crónica, destrucción de las células beta pancreáticas, osteoartritis, espondilitis reumatoidea, artiritis gotosa, enfermedad inflamatoria intestinal, síndrome de distrés respiratorio del adulto [ARDS, por sus siglas en inglés], soriasis, enfermedad de Crohn, rinitis alérgica, colitis ulcerosa, anafilaxis, dermatitis por contacto, asma, degeneración muscular, caquexia, síndrome de Reiter, diabetes del tipo I y del tipo II, enfermedades relacionadas con la resorción ósea, reacción injerto contra huésped, Mal de Alzheimer, ataque cerebrovascular, infarto del miocardio, lesión por isquemia-reperfusión, ateroesclerosis, trauma cerebral, esclerosis múltiple, malaria cerebral, sepsis, choque séptico, síndrome de choque tóxico, fiebre, mialgias padecidas a raíz de infecciones por VIH-1, VIH-2, VIH-3, citomegalovirus [CMV], gripe, adenovirus, herpes viral o infección por herpes zóster en un mamífero, que comprende la administración de una cantidad eficaz de un compuesto tal como el que se describió previamente.
ARP030101777A 2002-05-21 2003-05-22 Compuestos heterociclicos sustituidos y metodos de empleo AR039842A1 (es)

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US38269902P 2002-05-21 2002-05-21
US10/438,553 US7026326B2 (en) 2002-05-21 2003-05-13 Substituted heterocyclic compounds and methods of use

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US (1) US7026326B2 (es)
EP (1) EP1506186A1 (es)
JP (2) JP4606161B2 (es)
AR (1) AR039842A1 (es)
AU (1) AU2003234628B2 (es)
CA (1) CA2485166A1 (es)
MX (1) MXPA04011470A (es)
PL (1) PL376575A1 (es)
TW (1) TW200406399A (es)
WO (1) WO2003099808A1 (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2533684A1 (en) * 2003-07-25 2005-02-10 Amgen Inc. Substituted pyridones and pyrimidinones with antiinflammatory properties
US7429594B2 (en) 2003-08-20 2008-09-30 Amgen Inc. Substituted heterocyclic compounds and methods of use
US20080312281A1 (en) * 2004-12-24 2008-12-18 Matthew Colin Thor Fyfe G-Protein Coupled Receptor (Gpr116) Agonists and Use Thereof for Treating Obesity and Diabetes
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
US8062824B2 (en) * 2006-07-17 2011-11-22 E. I. Du Pont De Nemours And Company Thermally imageable dielectric layers, thermal transfer donors and receivers
US7528448B2 (en) * 2006-07-17 2009-05-05 E.I. Du Pont De Nemours And Company Thin film transistor comprising novel conductor and dielectric compositions
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
CN101801951B (zh) 2007-09-14 2013-11-13 杨森制药有限公司 1’,3’-二取代的-4-苯基-3,4,5,6-四氢-2h,1’h-[1,4’]二吡啶-2’-酮
US7666567B2 (en) 2007-10-23 2010-02-23 E. I. Du Pont De Nemours And Company Negative imaging method for providing a patterned metal layer having high conductivity
US7666568B2 (en) * 2007-10-23 2010-02-23 E. I. Du Pont De Nemours And Company Composition and method for providing a patterned metal layer having high conductivity
RU2510396C2 (ru) 2008-09-02 2014-03-27 Янссен Фармасьютикалз, Инк. 3-азабицикло[3.1.0]гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов
AU2009319387B2 (en) 2008-11-28 2012-05-10 Addex Pharma S.A. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
JP5707390B2 (ja) 2009-05-12 2015-04-30 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 １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体の正のアロステリック調節因子としてのその使用
RS53075B (en) 2009-05-12 2014-04-30 Janssen Pharmaceuticals Inc. 1,2,4-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
EP2661435B1 (en) 2010-11-08 2015-08-19 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2649069B1 (en) 2010-11-08 2015-08-26 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
ES2543050T3 (es) 2011-02-28 2015-08-14 Array Biopharma, Inc. Inhibidores de serina/treonina quinasa
US9187462B2 (en) 2011-08-04 2015-11-17 Array Biopharma Inc. Substituted quinazolines as serine/threonine kinase inhibitors
EP2773207B1 (en) * 2011-10-31 2018-03-07 Merck Sharp & Dohme Corp. Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
US10531655B2 (en) 2011-12-02 2020-01-14 The Regents Of The University Of California Reperfusion protection solution and uses thereof
SI2820009T1 (en) * 2012-03-01 2018-05-31 Array Biopharma, Inc. Serine / Threonine kinase inhibitors
BR112015004548A2 (pt) 2012-08-27 2017-08-08 Array Biopharma Inc inibidores de serina/treonina para tratamento de doenças hiperproliferativas
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
DK3431106T3 (da) 2014-01-21 2021-03-15 Janssen Pharmaceutica Nv Kombinationer omfattende positive allosteriske modulatorer eller orthosteriske agonister af metabotrop glutamaterg subtype 2-receptor og anvendelse af disse
ES2860298T3 (es) 2014-01-21 2021-10-04 Janssen Pharmaceutica Nv Combinaciones que comprenden moduladores alostéricos positivos del receptor glutamatérgico metabotrópico de subtipo 2 y su uso
MY190386A (en) 2017-04-11 2022-04-20 Mitsui Chemicals Agro Inc Pyridone compounds and agricultural and horticultural fungicides containing the same as active ingredients
ES2910839T3 (es) * 2017-08-23 2022-05-13 Sprint Bioscience Ab Compuestos de piridilpiridona
US11208423B2 (en) * 2017-08-23 2021-12-28 Sprint Bioscience Ab Pyridinamine-pyridone and pyrimidinamine- pyridone compounds
CN117083064A (zh) 2020-11-25 2023-11-17 德西费拉制药有限责任公司 作为vps34抑制剂用于治疗病毒感染的吡啶基吡啶酮衍生物
WO2023156386A2 (en) * 2022-02-16 2023-08-24 Duke Street Bio Limited Pharmaceutical compound

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2602794A (en) * 1952-07-08 Process for preparation of x-amino-s
WO1995009917A1 (en) 1993-10-07 1995-04-13 The Regents Of The University Of California Genetically engineered bispecific tetravalent antibodies
CA2205572A1 (en) 1994-12-12 1996-06-20 Beth Israel Hospital Association Chimeric cytokines and uses thereof
NZ503548A (en) 1996-02-09 2001-09-28 Amgen Inc A fusion protein comprising an IL-1ra receptor antagonist with a constant domain of human immunoglobulin at the carboxy terminus
US6100071A (en) 1996-05-07 2000-08-08 Genentech, Inc. Receptors as novel inhibitors of vascular endothelial growth factor activity and processes for their production
US6096753A (en) * 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6410729B1 (en) * 1996-12-05 2002-06-25 Amgen Inc. Substituted pyrimidine compounds and methods of use
TW520362B (en) * 1996-12-05 2003-02-11 Amgen Inc Substituted pyrimidine compounds and pharmaceutical composition comprising same
EP0948496A2 (en) * 1996-12-05 1999-10-13 Amgen inc. Substituted pyrimidinone and pyridone compounds and methods of use
EP2002846B1 (en) 1996-12-06 2017-01-25 Amgen Inc. Combination therapy using an IL-1 inhibitor for treating IL-1 mediated diseases
KR19980066046A (ko) 1997-01-18 1998-10-15 정용훈 고역가의 CTLA4-Ig 융합단백질
ES2183351T3 (es) 1997-04-17 2003-03-16 Amgen Inc Composicones que comprenden conjugados de proteina ob humana activa estable con una cadena fc de inmunoglobulinas y metodos.
NZ528409A (en) * 2001-03-15 2005-11-25 Basf Ag 5-phenylpyrimidine, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi

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