AR045083A1 - Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamento - Google Patents

Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamento

Info

Publication number
AR045083A1
AR045083A1 ARP040102612A ARP040102612A AR045083A1 AR 045083 A1 AR045083 A1 AR 045083A1 AR P040102612 A ARP040102612 A AR P040102612A AR P040102612 A ARP040102612 A AR P040102612A AR 045083 A1 AR045083 A1 AR 045083A1
Authority
AR
Argentina
Prior art keywords
methyl
pyrid
group
substituted
chosen
Prior art date
Application number
ARP040102612A
Other languages
English (en)
Original Assignee
Aventis Pharma Sa
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 Aventis Pharma Sa filed Critical Aventis Pharma Sa
Publication of AR045083A1 publication Critical patent/AR045083A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)

Abstract

Un producto que responde al grupo de fórmula (1), en la que:1) i) A, B, U, V, W, X, Y pueden ser N, C ó CR4; ó ii) A, B U, pueden ser N, C ó CR4; V y W son CH2, X se elige entre S, SO y SO2; e Y es una unión; 2) L-G-R1 se escoge entre un grupo de fórmula (2), 3); E es CR4, N, NR4 o S; 4) R1 y R2 se seleccionan independientemente en el grupo constituido por arilo, heteroarilo, arilo sustituido y heteroarilo sustituido; 5) L se selecciona en el grupo constituido por C=O, C=S, y C=N(R7); 6) R3 se selecciona en el grupo constituido por halógeno, CF3, CN, NO2, alquilo (C1-3), alquenilo (C1-3), alquinilo (C1-3), O-R7, S-R7, SO-R7, SO2-(R7), N(R7)(R8), halógeno, CO-OR7, CO-N(R7)(R8), SO2-N(R7)(R8), NR7-CO-R8 y BR7-SO2-alquilo(C1-3); 7) n = 0, 1, 2 ó 3; bien entendido que cuando n es superior a 1, los radicales R3 pueden ser idénticos o diferentes, y cuando n = 2, X e Y no están simultáneamente sustituidos con R3; 8) R4 se selecciona en el grupo constituido por H y alquilo (C1-3); 9) R5 y R6 se seleccionan independientemente en el grupo constituido por H y alquilo (C1-3); 10) R7 y, R8 se seleccionan independientemente en el grupo constituido por H, alquilo (C1-3) y alquilo (C1-3) sustituido; en forma racémica, enriquecida en un enantiómero, enriquecida en un diastereoisómero, sus tautómeros, sus profármacos y sus sales aceptables farmacéuticamente, a reserva de que el producto de grupo de fórmula (1) no sea uno de los compuestos (eventualmente salificados) de fórmula (3), en el que: i) R1 se escoge entre pirid-2-ilo o pirid-2-ilo sustituido, cada uno eventualmente en forma de N-óxido; R2 se escoge entre tien-2-ilo, pirid-2-ilo, pirid-3-ilo, pirid-4-ilo, fenilo, fenilo sustituido con al menos un sustituyente escogido entre F, OH, CF3, Me, OMe o NO2, en el que cuando R2 es pirid-2-ilo, pirid-3-ilo o pirid-4-ilo, R2 puede estar presente en forma de N-óxido; R4 se escoge entre metilo, 2-fluoroetilo o etilo; T y U se escogen independientemente entre H, metilo, Cl o F; o bien ii) R1 se escoge entre pirid-3-ilo o pirid-4-ilo; R2 se escoge entre tien-2-ilo o fenilo; R4 se escoge entre metilo o 2-fluoroetilo; T y U se escogen independientemente entre H, metilo, Cl o F; iii) R1 es pirid-2-ilo sustituido en posición 5 por un sustituyente tetrazolilo o amida, eventualmente sustituidos; R2 es fenilo; R4 es metilo; T es 5-metilo; U es H; iv) R1 es pirazin-2-ilo sustituido en posición 5 por CH2CONH2 o amida eventualmente sustituido; R2 es fenilo; R4 es metilo; T es elige entre 5-metil, 5-cloro, 5-fluoro y 5-bromo; U es H, o una fórmula (4), en el que: n es 2 ó 3; Het es 4-metil-tiazol-5-ilo ó imidazol-1-ilo; R2 es fenilo; R4 es metilo; T, Q, y Z se eligen independientemente entre N y CH, y R14 es H ó metilo; en el que: cuando T es N, entonces Q y Z son CH y R14 es H; cuando Q es N, y T y Z son CH, entonces R14 es H ó metilo; y cuando T es CH, entonces R14 es H. Composiciones que los contienen y su utilización para la fabricación de medicamentos con actividad anticancerosa.
ARP040102612A 2003-07-24 2004-07-22 Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamento AR045083A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0309092A FR2857966A1 (fr) 2003-07-24 2003-07-24 Produits aryl-heteroaromatiques, compositions les contenant et utilisation

Publications (1)

Publication Number Publication Date
AR045083A1 true AR045083A1 (es) 2005-10-12

Family

ID=33561081

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102612A AR045083A1 (es) 2003-07-24 2004-07-22 Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamento

Country Status (14)

Country Link
US (1) US20050020593A1 (es)
EP (1) EP1651602A2 (es)
JP (1) JP2006528615A (es)
KR (1) KR20060041274A (es)
CN (1) CN1826319A (es)
AR (1) AR045083A1 (es)
AU (1) AU2004259112A1 (es)
BR (1) BRPI0412254A (es)
CA (1) CA2533494A1 (es)
FR (1) FR2857966A1 (es)
IL (1) IL173205A0 (es)
MX (1) MXPA06000479A (es)
TW (1) TW200524907A (es)
WO (1) WO2005009947A2 (es)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
AU2005286728A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
MX2007003318A (es) 2004-09-20 2007-05-18 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
JP4958785B2 (ja) * 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用
AU2005286790A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-CoA-desaturase (SCD)
EP1827438B2 (en) * 2004-09-20 2014-12-10 Xenon Pharmaceuticals Inc. Piperazin derivatives for inhibiting human stearoyl-coa-desaturase
AU2005286648A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
CN101084211A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为治疗剂的用途
AR051094A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
US7767677B2 (en) 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20060293345A1 (en) * 2005-05-20 2006-12-28 Christoph Steeneck Heterobicyclic metalloprotease inhibitors
WO2007130075A1 (en) * 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
WO2007035620A2 (en) * 2005-09-16 2007-03-29 Serenex, Inc. Carbazole derivatives
CA2648748A1 (en) * 2006-04-14 2007-10-25 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound
ITMI20062230A1 (it) * 2006-11-22 2008-05-23 Acraf Composto 2-alchil-indazolico procedimento per preparalo e composizione farmaceutica che lo comprende
CN100444842C (zh) * 2006-11-30 2008-12-24 四川大学华西医院 N-芳基杂环族化合物的制药用途
NZ582056A (en) * 2007-08-10 2012-08-31 Lundbeck & Co As H Bicyclic heteroaryl compounds for treating conditions related to p2x7 receptor activation
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
EP2090576A1 (en) 2008-02-01 2009-08-19 Merz Pharma GmbH & Co.KGaA 6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators
AR077428A1 (es) * 2009-07-29 2011-08-24 Sanofi Aventis (aza) indolizinacarboxamidas ciclicas su preparacion y su uso como agentes farmaceuticos
WO2012173952A1 (en) 2011-06-13 2012-12-20 Emory University Piperazine derivatives, compositions, and uses related thereto
KR20150119370A (ko) 2013-02-19 2015-10-23 화이자 인코포레이티드 Cns 장애 및 다른 장애의 치료를 위한 pde4 동종효소의 억제제로서의 아자벤즈이미다졸 화합물
WO2014187922A1 (en) * 2013-05-24 2014-11-27 Iomet Pharma Ltd. Slc2a transporter inhibitors
CA2938311C (en) 2014-02-03 2023-03-07 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ror-gamma
EP2966856B1 (en) * 2014-07-08 2020-04-15 Sony Depthsensing Solutions N.V. A high dynamic range pixel and a method for operating it
WO2016012896A1 (en) 2014-07-24 2016-01-28 Pfizer Inc. Pyrazolopyrimidine compounds
HUE044040T2 (hu) 2014-08-06 2019-09-30 Pfizer Imidazopiridazin vegyületek
CN107074852B (zh) 2014-10-14 2019-08-16 生命医药有限责任公司 ROR-γ的二氢吡咯并吡啶抑制剂
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
CN104876851A (zh) * 2015-05-15 2015-09-02 南京大学 一类含吲哚-3羧酸骨架的哌嗪类衍生物的制备方法及在抗癌药物中的应用
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
EP3377482B1 (en) 2015-11-20 2021-05-12 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
CA3019145A1 (en) 2016-03-28 2017-10-05 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
KR20200053481A (ko) 2017-07-24 2020-05-18 비타이 파마슈티컬즈, 엘엘씨 RORγ의 억제제
US20210299117A1 (en) * 2018-08-06 2021-09-30 Moexa Pharmaceuticals Limited SMAD3 Inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPR283801A0 (en) * 2001-02-01 2001-03-01 Australian National University, The Chemical compounds and methods
DE10152306A1 (de) * 2001-10-26 2003-07-24 Asta Medica Ag 2-Acylindolderivate mit neuen therapeutisch wertvollen Eigenschaften
EP1452525A4 (en) * 2001-10-30 2005-01-26 Nippon Shinyaku Co Ltd AMIDE DERIVATIVES AND CORRESPONDING MEDICAMENTS

Also Published As

Publication number Publication date
EP1651602A2 (fr) 2006-05-03
MXPA06000479A (es) 2006-04-05
IL173205A0 (en) 2006-06-11
KR20060041274A (ko) 2006-05-11
WO2005009947A2 (fr) 2005-02-03
WO2005009947A3 (fr) 2005-03-31
FR2857966A1 (fr) 2005-01-28
TW200524907A (en) 2005-08-01
BRPI0412254A (pt) 2006-09-19
CN1826319A (zh) 2006-08-30
JP2006528615A (ja) 2006-12-21
AU2004259112A1 (en) 2005-02-03
CA2533494A1 (fr) 2005-02-03
US20050020593A1 (en) 2005-01-27

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