AR045083A1 - Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamento - Google Patents
Productos aril-heteroaromaticos, composiciones que los contienen y utilizacion como medicamentoInfo
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; 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
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[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
- C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic 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
- C07D513/02—Heterocyclic 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
- C07D513/04—Ortho-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.
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)
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)
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 |
-
2003
- 2003-07-24 FR FR0309092A patent/FR2857966A1/fr active Pending
-
2004
- 2004-07-22 AR ARP040102612A patent/AR045083A1/es unknown
- 2004-07-22 EP EP04785992A patent/EP1651602A2/fr not_active Withdrawn
- 2004-07-22 KR KR1020067001553A patent/KR20060041274A/ko not_active Application Discontinuation
- 2004-07-22 BR BRPI0412254-2A patent/BRPI0412254A/pt not_active Application Discontinuation
- 2004-07-22 WO PCT/FR2004/001944 patent/WO2005009947A2/fr not_active Application Discontinuation
- 2004-07-22 AU AU2004259112A patent/AU2004259112A1/en not_active Abandoned
- 2004-07-22 CN CNA2004800213553A patent/CN1826319A/zh active Pending
- 2004-07-22 MX MXPA06000479A patent/MXPA06000479A/es not_active Application Discontinuation
- 2004-07-22 JP JP2006520863A patent/JP2006528615A/ja active Pending
- 2004-07-22 CA CA002533494A patent/CA2533494A1/fr not_active Abandoned
- 2004-07-23 US US10/898,517 patent/US20050020593A1/en not_active Abandoned
- 2004-07-23 TW TW093121981A patent/TW200524907A/zh unknown
-
2006
- 2006-01-17 IL IL173205A patent/IL173205A0/en unknown
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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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |