YU35100A - 1,3-disupstituisane uree kao inhibitori enzima holesterol aciltransferaze (acat), i postupak za njihovo dobijanje - Google Patents

1,3-disupstituisane uree kao inhibitori enzima holesterol aciltransferaze (acat), i postupak za njihovo dobijanje

Info

Publication number
YU35100A
YU35100A YU35100A YU35100A YU35100A YU 35100 A YU35100 A YU 35100A YU 35100 A YU35100 A YU 35100A YU 35100 A YU35100 A YU 35100A YU 35100 A YU35100 A YU 35100A
Authority
YU
Yugoslavia
Prior art keywords
preparing
disubstituted ureas
acat inhibitors
isocyanates
enzyme
Prior art date
Application number
YU35100A
Other languages
English (en)
Inventor
Vladimir Oremus
Vendelin Smahovsky
Viera Faberova
Ivan Kakalik
Ludmila Schmidtova
Marian Zemanek
Original Assignee
Slovakofarma A.S.
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 Slovakofarma A.S. filed Critical Slovakofarma A.S.
Publication of YU35100A publication Critical patent/YU35100A/sh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D213/60—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 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 ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/32—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
    • C07C275/34—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C275/36—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with at least one of the oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. N-aryloxyphenylureas
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/43—Y being a hetero atom
    • C07C323/44—X or Y being nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Pronalazak se odnosi na 1,3-disupstituisane uree sa opštom formulom (I) gde je R1 aril, R2 nitro i/ili amino, i X je kiseonik i/ili sumpor, i postupak za njihovo dobijanje koji se sastoji u tretiranju aromatičnih amina sa izocijanatima. Izocijanati se mogu dobiti in situ i reakcija se izvršava u toluenu na 80В°C. Ukoliko se formira nitrogrupa, ona se redukuje sa vodonikom u prisustvu paladijumskog katalizatora na amino grupi. Dobijeni 1,3-disupstituisane uree su inhibitori aktivnosti acil koenzima A. enzima holesterol aciltransferaze (ACAT) i mogu se koristiti za inhibiranje esterifikacije holesterola i za apsorpciju u hiperholesterolemije.[The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80В°C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.
YU35100A 1997-12-19 1998-12-16 1,3-disupstituisane uree kao inhibitori enzima holesterol aciltransferaze (acat), i postupak za njihovo dobijanje YU35100A (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SK1751-97A SK282727B6 (sk) 1997-12-19 1997-12-19 1,3-Disubstituované močoviny - inhibítory ACAT a spôsob ich prípravy

Publications (1)

Publication Number Publication Date
YU35100A true YU35100A (sh) 2002-10-18

Family

ID=20434795

Family Applications (1)

Application Number Title Priority Date Filing Date
YU35100A YU35100A (sh) 1997-12-19 1998-12-16 1,3-disupstituisane uree kao inhibitori enzima holesterol aciltransferaze (acat), i postupak za njihovo dobijanje

Country Status (18)

Country Link
US (1) US6444691B1 (sh)
EP (1) EP1042278B1 (sh)
JP (1) JP2001526259A (sh)
AT (1) ATE233727T1 (sh)
AU (1) AU1697699A (sh)
BG (1) BG104537A (sh)
CZ (1) CZ299695B6 (sh)
DE (1) DE69811949T2 (sh)
DK (1) DK1042278T3 (sh)
ES (1) ES2194379T3 (sh)
HR (1) HRP20000351B1 (sh)
HU (1) HUP0004332A3 (sh)
PL (1) PL341235A1 (sh)
PT (1) PT1042278E (sh)
RU (1) RU2216536C2 (sh)
SK (1) SK282727B6 (sh)
WO (1) WO1999032437A1 (sh)
YU (1) YU35100A (sh)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2377847T3 (es) 1999-01-13 2012-04-02 Bayer Healthcare Llc Difenil ureas sustituidas con omega-carboxi arilo como agentes inhibidores de la cinasa p38
US7928239B2 (en) * 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
SI1478358T1 (sl) 2002-02-11 2013-09-30 Bayer Healthcare Llc Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi
EP1474393A1 (en) 2002-02-11 2004-11-10 Bayer Pharmaceuticals Corporation Aryl ureas as kinase inhibitors
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
EP1608319A4 (en) 2003-04-03 2007-02-28 Univ California IMPROVED HEMMER FOR SOLUBLE EPOXY HYDROLASE
DK1626714T3 (da) 2003-05-20 2007-10-15 Bayer Pharmaceuticals Corp Dirarylurinstoffer mod sygdomme medieret af PDGFR
RS52625B (en) 2003-07-23 2013-06-28 Bayer Healthcare Llc FLUORO SUBSTITUTED OMEGA-CARBOXYARYL DIPHENYL UREA FOR TREATMENT AND PREVENTION OF DISEASES AND DISEASES
WO2005068420A1 (en) * 2003-12-23 2005-07-28 Esperion Therapeutics, Inc. Urea and thiourea compounds and compositions for cholesterol management and related uses
JP2007532484A (ja) 2004-03-16 2007-11-15 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 可溶性エポキシド加水分解酵素の阻害剤およびエポキシエイコサノイドを用いて腎症を緩和する方法
CA2584342C (en) * 2004-10-20 2013-04-30 The Regents Of The University Of California Improved inhibitors for the soluble epoxide hydrolase
SK287385B6 (sk) 2007-11-27 2010-08-09 Hameln-Rds, A. S. 1,3-Disubstituované močoviny, spôsob ich prípravy a použitia
HRP20090186A2 (hr) 2009-03-31 2010-10-31 Institut Ruđer Bošković Adamantanski bisureidni derivati, metoda priprave i primjena u detekciji aniona
CN102869261A (zh) * 2010-03-01 2013-01-09 瑞科西有限公司 化合物及其治疗应用
US8912184B1 (en) 2010-03-01 2014-12-16 Alzheimer's Institute Of America, Inc. Therapeutic and diagnostic methods
RU2486893C1 (ru) * 2012-06-13 2013-07-10 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Волгоградский государственный технический университет" (ВолгГТУ) Способ получения бис[3-метил(адамант-1-ил)]мочевин
CN107417478B (zh) * 2017-06-05 2020-05-05 南京师范大学 一种催化氧化羰基化合成不对称二取代脲的方法
CN115677660B (zh) * 2022-10-27 2024-05-03 中国药科大学 苯基脲类化合物及其制备方法、用途和药物组合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3284433A (en) * 1963-07-17 1966-11-08 Merck & Co Inc 4-phenoxy-carbanilides
FR1593586A (sh) * 1967-10-17 1970-06-01
DE2246109A1 (de) * 1972-09-20 1974-03-28 Bayer Ag 1-(4-phenoxy-phenyl)-1,3,5-triazinderivate, ein verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
JP2720053B2 (ja) * 1988-11-09 1998-02-25 チッソ株式会社 新規なジアミノ化合物、ジニトロ化合物、ジオール化合物および製造方法
FR2674522B1 (fr) 1991-03-26 1993-07-16 Lipha Nouveaux derives de l'indole, procedes de preparation et medicaments les contenant.
JP3668266B2 (ja) 1994-02-01 2005-07-06 株式会社日清製粉グループ本社 尿素誘導体
US5576335A (en) 1994-02-01 1996-11-19 Nisshin Flour Milling Co., Ltd. Urea derivatives and their use as ACAT inhibitors
CA2161376C (en) 1994-10-27 2005-01-11 Toshiaki Minami Reversible multi-color thermal recording medium

Also Published As

Publication number Publication date
DE69811949T2 (de) 2004-03-04
DE69811949D1 (de) 2003-04-10
HUP0004332A2 (hu) 2001-05-28
EP1042278A1 (en) 2000-10-11
SK175197A3 (en) 1999-07-12
CZ20002297A3 (cs) 2000-11-15
PL341235A1 (en) 2001-03-26
CZ299695B6 (cs) 2008-10-22
DK1042278T3 (da) 2003-06-30
HUP0004332A3 (en) 2002-11-28
JP2001526259A (ja) 2001-12-18
RU2216536C2 (ru) 2003-11-20
HRP20000351B1 (en) 2003-10-31
WO1999032437A1 (en) 1999-07-01
SK282727B6 (sk) 2002-11-06
BG104537A (en) 2000-12-29
US6444691B1 (en) 2002-09-03
ATE233727T1 (de) 2003-03-15
HRP20000351A2 (en) 2000-12-31
AU1697699A (en) 1999-07-12
ES2194379T3 (es) 2003-11-16
PT1042278E (pt) 2003-07-31
EP1042278B1 (en) 2003-03-05

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