AR050189A1 - Derivados sustituidos de propenil piperazina como inhibidores de histona desacetilasa - Google Patents
Derivados sustituidos de propenil piperazina como inhibidores de histona desacetilasaInfo
- Publication number
- AR050189A1 AR050189A1 ARP050103145A ARP050103145A AR050189A1 AR 050189 A1 AR050189 A1 AR 050189A1 AR P050103145 A ARP050103145 A AR P050103145A AR P050103145 A ARP050103145 A AR P050103145A AR 050189 A1 AR050189 A1 AR 050189A1
- Authority
- AR
- Argentina
- Prior art keywords
- quinoline
- alkyl
- alkyloxy
- independently selected
- mono
- 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
- C07D401/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente trata de compuestos que poseen actividad inhibitoria de la enzima histona desacetilasa; su preparacion, composiciones que los contienen y su uso como medicamento. Reivindicaion 1: Un compuesto de formula (1), las formas N-oxidos, las sales de adicion con ácidos aceptables para uso farmacéutico y las formas estereoquímicamente isoméricas del mismo, en el cual cada X es independientemente N o CH; R1 es fenilo, naftalenilo o heterociclilo; donde cada uno de dichos fenilo o naftalenilo está opcionalmente sustituido con uno o dos sustituyentes, cada uno seleccionado idependientemente a partir de halo, alquilo C1-6, alquiloxi C1-6, polihaloalquilo C1-6, arilo, hidroxi, ciano, amino, alquil C1-6carbonilamino, alquilsulfonilamino C1-6, hidroxicarbonilo, alquiloxi C1-6carbonilo, hidroxialquilo C1-6, alquiloxi C1-6metilo, aminometilo, alquil C1-6aminometilo, alquil C1-6carbonilaminometilo, alquil C1-6sulfonilaminometilo, aminosulfonilo, alquil C1- 6aminosulfonilo o heterociclilo, R2 es H, -CH2-R5, trifluorometilo, -C(=O)-R6, o -CH2-NR7R8; donde cada R5 se selecciona independientemente de H, hidroxi, alquiloxi C1-6, alquiloxi C1-6alquiloxi C1-6, alquil C1-6carboniloxi, piperazinilo, N- metilpiperazinilo, morfolinilo, tiomorfolinilo, imidazolilo o triazolilo; cada R6 se selecciona independientemente de hidroxi, alquiloxi C1-6, amino o mono- o di(alquil C1-6)amino, cicloalquilamino C1-6, hidroxialquilamino C1-6, piperazinilo, mono- o di(alquil C1-6)aminoalquilamino C1-6, N-metilpiperazinilo, morfolinilo o tiomorfolinilo; cada R7 y R8 se seleccionan independientemente de H, alquilo C1-6, alquil C1-6carbonilo, alquilsulfonilo C1-6, o mono- o di(alquil C1-6)aminosulfonilo; R3 es H, hidroximetilo, aminometilo o mono- o di(alquil C1-6)aminometilo; R4 es H o alquilo C1-6; arilo como se meciona anteriormente es fenilo o naftalenilo; donde cada uno de dichos fenilo o naftalenilo está opcionalmente sustituido con uno o dos sustituyentes, cada uno seleccionado independientemente de halo, alquilo C1-6, alquiloxi C1-6, trifluorometilo, ciano o hidroxicarbonilo; y heterociclilo en los anteriores es furanilo, tienilo, pirrolilo, pirrolinilo, pirolidinilo, dioxolilo, oxazolilo, tiazolilo, imidazolilo, imidazolinilo, imidazolidinilo, pirazolilo, pirazolinilo, pirazolidinilo, isoxazolilo, isotiazolilo, oxadiazolilo, triazolilo, tiadiazolilo, piranilo, piridinilo, piperidinilo, dioxanilo, morfolinilo, titianilo, tiomorfolinilo, piridacinilo, pirimidinilo,piracinilo, piperazinilo, triacinilo, tritianilo, indolizinilo, indolilo, indolinilo, benzofuranilo, benzotiofenilo, indazolilo, benzoimidazolilo, benzotiazolilo, purinilo, quinozinilo, quinolinilo, cinolinilo, ftalazinilo, quinazolinilo, quinoxalinilo o naftiridinilo; donde cada uno de dichos heteociclos está opcionalmente sustituido con uno o dos sustituyentes, cada uno seleccionado inependientemente de halo, alquilo C1-6, alquiloxi C1-6, ciano, amino, mono- o di(alquil C1-4)amino.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04077171 | 2004-07-28 | ||
| US59235704P | 2004-07-29 | 2004-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050189A1 true AR050189A1 (es) | 2006-10-04 |
Family
ID=39294123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103145A AR050189A1 (es) | 2004-07-28 | 2005-07-28 | Derivados sustituidos de propenil piperazina como inhibidores de histona desacetilasa |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP1776358B1 (es) |
| JP (1) | JP5279268B2 (es) |
| KR (1) | KR101282833B1 (es) |
| CN (1) | CN1993356B (es) |
| AR (1) | AR050189A1 (es) |
| AT (1) | ATE432274T1 (es) |
| AU (1) | AU2005266311B2 (es) |
| BR (1) | BRPI0513891B8 (es) |
| CA (1) | CA2572971C (es) |
| CY (1) | CY1110358T1 (es) |
| DE (1) | DE602005014646D1 (es) |
| DK (1) | DK1776358T3 (es) |
| EA (1) | EA011932B1 (es) |
| ES (1) | ES2327253T3 (es) |
| HK (1) | HK1106236A1 (es) |
| HR (1) | HRP20090439T1 (es) |
| IL (1) | IL180961A0 (es) |
| MX (1) | MX2007001119A (es) |
| MY (1) | MY142831A (es) |
| NO (1) | NO20071117L (es) |
| NZ (1) | NZ552758A (es) |
| PL (1) | PL1776358T3 (es) |
| PT (1) | PT1776358E (es) |
| SI (1) | SI1776358T1 (es) |
| TW (1) | TWI394752B (es) |
| WO (1) | WO2006010749A2 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE396971T1 (de) | 2002-03-13 | 2008-06-15 | Janssen Pharmaceutica Nv | Sulfonylaminoderivate als neue inhibitoren von histondeacetylase |
| WO2003076438A1 (en) | 2002-03-13 | 2003-09-18 | Janssen Pharmaceutica N.V. | Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase |
| WO2003075929A1 (en) | 2002-03-13 | 2003-09-18 | Janssen Pharmaceutica N.V. | Inhibitors of histone deacetylase |
| EA010652B1 (ru) | 2004-07-28 | 2008-10-30 | Янссен Фармацевтика Н.В. | Замещенные индолильные алкиламинопроизводные в качестве новых ингибиторов гистондеацетилазы |
| DK1885710T3 (en) | 2005-05-18 | 2015-11-23 | Janssen Pharmaceutica Nv | SUBSTITUTED AMINOPROPENYLPIPERIDINE OR MORPHOLINE DERIVATIVES AS UNKNOWN INHIBITORS OF HISTONDEACETYLASE |
| WO2007049262A1 (en) * | 2005-10-27 | 2007-05-03 | Berand Limited | Methods and compositions for the promotion of neuronal growth and the treatment of asociality and affective disorders |
| SI1981874T1 (sl) | 2006-01-19 | 2009-10-31 | Janssen Pharmaceutica Nv | Aminofenilni derivati kot novi inhibitorji histon deacetilaze |
| DK1981875T3 (da) | 2006-01-19 | 2014-07-14 | Janssen Pharmaceutica Nv | Substituerede indolylalkylaminoderivater som inhibitorer af histondeacetylase |
| WO2007082874A1 (en) * | 2006-01-19 | 2007-07-26 | Janssen Pharmaceutica N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
| JP5137848B2 (ja) | 2006-01-19 | 2013-02-06 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒストンデアセチラーゼのインヒビターとしてのピリジン及びピリミジン誘導体 |
| EP1839656A1 (en) * | 2006-03-31 | 2007-10-03 | TopoTarget Germany AG | Use of valproic acid for the topical treatment of mild to moderate acne vulgaris |
| KR20100095430A (ko) | 2007-11-02 | 2010-08-30 | 메틸진 인크. | 히스톤 탈아세틸화효소의 저해물질 |
| CN101723896B (zh) * | 2009-11-03 | 2012-10-31 | 山东大学 | 酪氨酸衍生物类组蛋白去乙酰化酶抑制剂及其应用 |
| WO2012117421A1 (en) | 2011-03-02 | 2012-09-07 | Orchid Research Laboratories Ltd | Histone deacetylase inhibitors |
| KR101419836B1 (ko) * | 2012-05-10 | 2014-07-16 | 서울대학교산학협력단 | Δ5-2-옥소피페라진 유도체를 포함하는 중간엽 줄기세포의 연골세포로의 분화 유도용 조성물 |
| KR101586045B1 (ko) | 2013-07-30 | 2016-01-15 | 충북대학교 산학협력단 | 신규 페닐티아졸 기반 히드록삼산 및 이를 유효성분으로 포함하는 항암용 조성물 |
| KR102132078B1 (ko) | 2018-09-20 | 2020-07-08 | 원광대학교산학협력단 | 방향족 화합물, 아민 및 친핵체를 이용한 3가지 성분 반응으로 1-에틸-4-페닐피페라진 유도체를 제조하는 방법 |
| KR20230155311A (ko) | 2022-05-03 | 2023-11-10 | 충북대학교 산학협력단 | 신규한 n-히드록시프로펜아미드 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물 |
| KR20230155310A (ko) | 2022-05-03 | 2023-11-10 | 충북대학교 산학협력단 | 신규한 n-히드록시프로펜아미드 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH17194A (en) * | 1980-03-06 | 1984-06-19 | Otsuka Pharma Co Ltd | Novel carbostyril derivatives,and pharmaceutical composition containing the same |
| WO2003076438A1 (en) * | 2002-03-13 | 2003-09-18 | Janssen Pharmaceutica N.V. | Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase |
| WO2003075929A1 (en) * | 2002-03-13 | 2003-09-18 | Janssen Pharmaceutica N.V. | Inhibitors of histone deacetylase |
| ATE399012T1 (de) * | 2002-04-03 | 2008-07-15 | Topotarget Uk Ltd | Carbaminsäurederivate enthaltend eine piperazin verknüpfung als hdac-inhibitoren |
-
2005
- 2005-07-25 AU AU2005266311A patent/AU2005266311B2/en active Active
- 2005-07-25 CA CA2572971A patent/CA2572971C/en active Active
- 2005-07-25 BR BRPI0513891A patent/BRPI0513891B8/pt active IP Right Grant
- 2005-07-25 PL PL05777776T patent/PL1776358T3/pl unknown
- 2005-07-25 AT AT05777776T patent/ATE432274T1/de active
- 2005-07-25 DK DK05777776T patent/DK1776358T3/da active
- 2005-07-25 MX MX2007001119A patent/MX2007001119A/es active IP Right Grant
- 2005-07-25 KR KR1020077001641A patent/KR101282833B1/ko active IP Right Grant
- 2005-07-25 ES ES05777776T patent/ES2327253T3/es active Active
- 2005-07-25 DE DE602005014646T patent/DE602005014646D1/de active Active
- 2005-07-25 PT PT05777776T patent/PT1776358E/pt unknown
- 2005-07-25 JP JP2007523072A patent/JP5279268B2/ja active Active
- 2005-07-25 CN CN2005800254878A patent/CN1993356B/zh active Active
- 2005-07-25 WO PCT/EP2005/053611 patent/WO2006010749A2/en active Application Filing
- 2005-07-25 EP EP05777776A patent/EP1776358B1/en active Active
- 2005-07-25 SI SI200530748T patent/SI1776358T1/sl unknown
- 2005-07-25 NZ NZ552758A patent/NZ552758A/en unknown
- 2005-07-25 EA EA200700143A patent/EA011932B1/ru unknown
- 2005-07-27 TW TW094125340A patent/TWI394752B/zh active
- 2005-07-28 AR ARP050103145A patent/AR050189A1/es active IP Right Grant
- 2005-07-28 MY MYPI20053492A patent/MY142831A/en unknown
-
2007
- 2007-01-25 IL IL180961A patent/IL180961A0/en active IP Right Grant
- 2007-02-27 NO NO20071117A patent/NO20071117L/no not_active Application Discontinuation
- 2007-10-30 HK HK07111697.6A patent/HK1106236A1/xx unknown
-
2009
- 2009-08-06 CY CY20091100839T patent/CY1110358T1/el unknown
- 2009-08-13 HR HR20090439T patent/HRP20090439T1/hr unknown
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Legal Events
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| FG | Grant, registration |