EA200200650A1 - Замещенные производные пиперазина в качестве ингибиторов мтр-протеина - Google Patents

Замещенные производные пиперазина в качестве ингибиторов мтр-протеина

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Publication number
EA200200650A1
EA200200650A1 EA200200650A EA200200650A EA200200650A1 EA 200200650 A1 EA200200650 A1 EA 200200650A1 EA 200200650 A EA200200650 A EA 200200650A EA 200200650 A EA200200650 A EA 200200650A EA 200200650 A1 EA200200650 A1 EA 200200650A1
Authority
EA
Eurasian Patent Office
Prior art keywords
mtp
piperazin
substituted derivatives
protein inhibitors
compounds
Prior art date
Application number
EA200200650A
Other languages
English (en)
Inventor
Армин Хеккель
Торстен Леманн-Линтц
Лео Томас
Михаэль Марк
Original Assignee
Бёрингер Ингельхайм Фарма Кг
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 Бёрингер Ингельхайм Фарма Кг filed Critical Бёрингер Ингельхайм Фарма Кг
Publication of EA200200650A1 publication Critical patent/EA200200650A1/ru

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    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
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    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
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    • C07—ORGANIC CHEMISTRY
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    • C07D219/00—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
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    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
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    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
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    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/80—Dibenzopyrans; Hydrogenated dibenzopyrans
    • C07D311/82—Xanthenes
    • C07D311/84—Xanthenes 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 in position 9
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    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В заявке описаны замещенные производные пиперазина общей формулы (I)в которой R-R, Y, Y, X и n имеют указанные в п.1 формулы изобретения значения, их изомеры и их соли, прежде всего их физиологически приемлемые соли, которые являются эффективными ингибиторами микросомального протеина-переносчика триглецирида (МТР-протеина), а также описаны содержащие эти соединения лекарственные средства и применение этих соединений, а также способ их получения.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200650A 1999-12-27 2000-12-16 Замещенные производные пиперазина в качестве ингибиторов мтр-протеина EA200200650A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19963235A DE19963235A1 (de) 1999-12-27 1999-12-27 Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
PCT/EP2000/012842 WO2001047899A1 (de) 1999-12-27 2000-12-16 Substituierte piperazinderivateals inhibitoren des mtp

Publications (1)

Publication Number Publication Date
EA200200650A1 true EA200200650A1 (ru) 2002-12-26

Family

ID=7934665

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200650A EA200200650A1 (ru) 1999-12-27 2000-12-16 Замещенные производные пиперазина в качестве ингибиторов мтр-протеина

Country Status (26)

Country Link
US (1) US20030114442A1 (ru)
EP (1) EP1259492A1 (ru)
JP (1) JP2003519131A (ru)
KR (1) KR20020065916A (ru)
CN (1) CN1414956A (ru)
AR (1) AR027112A1 (ru)
AU (1) AU2366001A (ru)
BG (1) BG106847A (ru)
BR (1) BR0016780A (ru)
CA (1) CA2394644A1 (ru)
CO (1) CO5251384A1 (ru)
CZ (1) CZ20022281A3 (ru)
DE (1) DE19963235A1 (ru)
EA (1) EA200200650A1 (ru)
EE (1) EE200200364A (ru)
HU (1) HUP0203855A3 (ru)
IL (1) IL150357A0 (ru)
MX (1) MXPA02006510A (ru)
NO (1) NO20023001L (ru)
PL (1) PL355394A1 (ru)
SK (1) SK9272002A3 (ru)
TR (1) TR200201669T2 (ru)
UY (1) UY26501A1 (ru)
WO (1) WO2001047899A1 (ru)
YU (1) YU49902A (ru)
ZA (1) ZA200205012B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100575944B1 (ko) 2001-06-28 2006-05-02 화이자 프로덕츠 인코포레이티드 미소체 트리글리세라이드 전달 단백질(ｍｔｐ) 및/또는아포지방단백질 ｂ(ａｐｏ ｂ)분비의 억제제로서의트리아미드-치환된 인돌, 벤조푸란 및 벤조티오펜
DE10200633A1 (de) * 2002-01-10 2003-07-24 Boehringer Ingelheim Pharma Kombination von MTP Inhibitoren oder apoB-Sekretions-Inhibitoren mit Fibraten zur Verwendung als Arzneimittel
SG165154A1 (en) * 2002-02-28 2010-10-28 Japan Tobacco Inc Ester compound and medical use thereof
EP1669345A4 (en) 2003-08-29 2008-02-20 Japan Tobacco Inc ESTER DERIVATIVE AND MEDICAL USE THEREOF
US20060030623A1 (en) * 2004-07-16 2006-02-09 Noboru Furukawa Agent for the treatment or prevention of diabetes, obesity or arteriosclerosis
US8101774B2 (en) * 2004-10-18 2012-01-24 Japan Tobacco Inc. Ester derivatives and medicinal use thereof
AU2005297923B2 (en) * 2004-10-25 2010-12-23 Japan Tobacco Inc. Solid medicinal preparation improved in solubility and stability and process for producing the same
EP2076487B1 (en) 2006-10-24 2010-05-26 Janssen Pharmaceutica N.V. Mtp inhibiting tetrahydro-naphthalene-1-carboxylic acid derivatives
JO2653B1 (en) * 2006-10-24 2012-06-17 شركة جانسين فارماسوتيكا ان. في Tetrahydroflavin 1-carboxylic acid substituted with pyridine or pyrazine inhibit MTB
US8138191B2 (en) 2007-01-11 2012-03-20 Critical Outcome Technologies Inc. Inhibitor compounds and cancer treatment methods
US8190707B2 (en) 2007-10-20 2012-05-29 Citrix Systems, Inc. System and method for transferring data among computing environments
WO2009079797A1 (en) 2007-12-26 2009-07-02 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
CA2999435A1 (en) 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5739135A (en) * 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5885983A (en) * 1996-05-10 1999-03-23 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
AU5513298A (en) * 1996-12-20 1998-07-17 Bristol-Myers Squibb Company Heterocyclic inhibitors of microsomal triglyceride transfer protein and method

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Publication number Publication date
BG106847A (en) 2003-02-28
TR200201669T2 (tr) 2002-10-21
MXPA02006510A (es) 2002-11-29
ZA200205012B (en) 2003-01-16
PL355394A1 (en) 2004-04-19
BR0016780A (pt) 2002-08-27
HUP0203855A3 (en) 2004-07-28
IL150357A0 (en) 2002-12-01
AR027112A1 (es) 2003-03-12
EE200200364A (et) 2003-10-15
CO5251384A1 (es) 2003-02-28
SK9272002A3 (en) 2002-11-06
EP1259492A1 (de) 2002-11-27
UY26501A1 (es) 2001-07-31
AU2366001A (en) 2001-07-09
CZ20022281A3 (cs) 2002-10-16
NO20023001D0 (no) 2002-06-21
CA2394644A1 (en) 2001-07-05
US20030114442A1 (en) 2003-06-19
HUP0203855A2 (hu) 2003-03-28
WO2001047899A1 (de) 2001-07-05
NO20023001L (no) 2002-06-21
YU49902A (sh) 2005-03-15
KR20020065916A (ko) 2002-08-14
JP2003519131A (ja) 2003-06-17
CN1414956A (zh) 2003-04-30
DE19963235A1 (de) 2001-07-05

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