BG101402A - Инхибитори на аполипопротеин-в синтеза - Google Patents

Инхибитори на аполипопротеин-в синтеза

Info

Publication number
BG101402A
BG101402A BG101402A BG10140297A BG101402A BG 101402 A BG101402 A BG 101402A BG 101402 A BG101402 A BG 101402A BG 10140297 A BG10140297 A BG 10140297A BG 101402 A BG101402 A BG 101402A
Authority
BG
Bulgaria
Prior art keywords
hydrogen
alkyl
apoliprotein
halo
cycloalkyl
Prior art date
Application number
BG101402A
Other languages
English (en)
Other versions
BG63694B1 (bg
Inventor
Jan Heeres
Leo Backx
Robert HENDRICKX
DER EYCKEN Luc VAN
CHAFFOY DE COURCELLES Didier DE
Original Assignee
Janssen Pharmaceutica N.V.
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
Priority claimed from US08/455,304 external-priority patent/US5521186A/en
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of BG101402A publication Critical patent/BG101402A/bg
Publication of BG63694B1 publication Critical patent/BG63694B1/bg

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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)
  • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Изобретението се отнася до нови съединения с общаформула (І), в която А и В заедно образуват бивалентен радикал с формула N=CH , -CH=N- , -CH2-CH2- , -CH=CH- , -C(=0)-CH2- , -CH2-C(0)- , R1 е водород, С1-6 алкил или халоген, R2 е водород или халоген, R3 означава водород, С1-8 алкил, С3-6 циклоалкил или С1-8 алкил, заместен с хидрокси, оксо, С3-6 циклоалкил или арил, Het е пет- или шестчленен евентуално заместен пръстен, до техни N-оксиди, стереохимични изомерни форми и фармацевтично приемливи присъединителни с киселина соли. Съединенията намират приложение в медицината, по-специално като понижаващо липидите средство. Изобретението се отнасясъщо до фармацевтични състави и до методи за получаването на съединенията и съставите.
BG101402A 1994-10-27 1997-04-10 Инхибитори на аполипопротеин-в синтеза BG63694B1 (bg)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP94203120 1994-10-27
US08/455,304 US5521186A (en) 1994-10-27 1995-05-31 Apolipoprotein-β synthesis inhibitors
PCT/EP1995/004111 WO1996013499A1 (en) 1994-10-27 1995-10-19 Apolipoprotein-b synthesis inhibitors

Publications (2)

Publication Number Publication Date
BG101402A true BG101402A (bg) 1997-10-31
BG63694B1 BG63694B1 (bg) 2002-09-30

Family

ID=26136684

Family Applications (1)

Application Number Title Priority Date Filing Date
BG101402A BG63694B1 (bg) 1994-10-27 1997-04-10 Инхибитори на аполипопротеин-в синтеза

Country Status (30)

Country Link
US (1) US5929075A (bg)
EP (1) EP0788496B1 (bg)
JP (1) JP3025907B2 (bg)
KR (1) KR100227231B1 (bg)
CN (1) CN1068000C (bg)
AP (1) AP779A (bg)
AT (1) ATE198889T1 (bg)
AU (1) AU697744C (bg)
BG (1) BG63694B1 (bg)
BR (1) BR9509436A (bg)
CA (1) CA2203274C (bg)
CY (1) CY2256B1 (bg)
CZ (1) CZ286476B6 (bg)
DE (3) DE122007000005I1 (bg)
DK (1) DK0788496T3 (bg)
ES (1) ES2155535T3 (bg)
FI (1) FI119548B (bg)
GR (1) GR3035519T3 (bg)
HR (1) HRP950532B1 (bg)
HU (1) HU219862B (bg)
IL (1) IL115771A (bg)
LU (1) LU91306I2 (bg)
NO (1) NO311937B1 (bg)
NZ (1) NZ295353A (bg)
OA (1) OA10479A (bg)
PT (1) PT788496E (bg)
RO (1) RO118715B1 (bg)
SK (1) SK281908B6 (bg)
TR (1) TR199501295A2 (bg)
WO (1) WO1996013499A1 (bg)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001521899A (ja) * 1997-11-03 2001-11-13 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 脂質低下剤組成物
CN1308523A (zh) * 1998-04-27 2001-08-15 詹森药业有限公司 含有用降脂剂和聚合物包衣的丸芯的微丸
WO2000037463A1 (en) * 1998-12-22 2000-06-29 Janssen Pharmaceutica N.V. S-oxide lipid lowering compounds
DE19945982A1 (de) * 1999-09-24 2001-03-29 Knoll Ag Geschwindigkeitsbestimmte Partikel
US20050132022A1 (en) * 2003-12-12 2005-06-16 International Business Machines Corporation Computer system with LAN-based I/O
CA2552988A1 (en) * 2004-01-21 2005-08-04 Janssen Pharmaceutica Nv Mitratapide oral solution
US7649002B2 (en) 2004-02-04 2010-01-19 Pfizer Inc (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists
US7262318B2 (en) * 2004-03-10 2007-08-28 Pfizer, Inc. Substituted heteroaryl- and phenylsulfamoyl compounds
EP1737460A2 (en) * 2004-04-09 2007-01-03 Janssen Pharmaceutica N.V. Intermittent dosing regimen for the treatment of overweight with mtp-inhibitors
US20050288340A1 (en) * 2004-06-29 2005-12-29 Pfizer Inc Substituted heteroaryl- and phenylsulfamoyl compounds
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
CA2609783A1 (en) * 2005-05-27 2006-12-07 Pfizer Products Inc. Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss
CA2617654A1 (en) * 2005-08-04 2007-02-08 Pfizer Limited Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
CA2642922C (en) * 2006-02-23 2011-08-02 Pfizer Limited Melanocortin type 4 receptor agonist piperidinoylpyrrolidines
US8383660B2 (en) 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
CN101583593A (zh) 2006-11-13 2009-11-18 辉瑞产品公司 二芳基、二吡啶基和芳基-吡啶基衍生物及其用途
JP5498168B2 (ja) 2006-12-01 2014-05-21 ブリストル−マイヤーズ スクイブ カンパニー アテローム性動脈硬化および循環器疾患の治療のためのｃｅｔｐ阻害剤としてのｎ−（（３−ベンジル）−２，２−（ビス−フェニル）−プロパン−１−アミン誘導体
JP5350367B2 (ja) * 2007-05-25 2013-11-27 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 （２ｓ−シス）−２−（ブロモメチル）−２−（４−クロロフェニル）−１，３−ジオキソラン−４−メタノールメタンスルホネート（エステル）の改良された合成
MX2011001405A (es) * 2008-08-06 2011-03-21 Pfizer Ltd Compuestos de diazepina y diazocano como agonistas de mc4.
US9040539B2 (en) * 2010-05-19 2015-05-26 Sandoz Ag Process for the preparation of chiral triazolones
MA54133B1 (fr) 2018-03-08 2022-01-31 Incyte Corp Composés d'aminopyrazine diol utilisés comme inhibiteurs de pi3k-y
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4313953A (en) * 1978-06-23 1982-02-02 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
US4218458A (en) * 1978-06-23 1980-08-19 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-aryloxy-methyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
US4766125A (en) * 1981-06-23 1988-08-23 Janssen Pharmaceutica N.V. N-aryl-piperazinealkanamides useful for protecting hearts from myocardial injury caused by ischaemia, anoxia or hypoxia
US4619931A (en) * 1983-02-28 1986-10-28 Janssen Pharmaceutica, N.V. [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles
CA1292472C (en) * 1985-12-03 1991-11-26 Alfonsus Guilielmus Knaeps Derivatives of ¬¬4-¬4-(4-phenyl-1-piperazinyl)- phenoxymethyl|-1,3-dioxolan-2-yl|methyl|-1h-imidazoles and 1h-1,2,4-triazoles
NZ223799A (en) * 1987-03-25 1989-12-21 Janssen Pharmaceutica Nv Azolylmethyl-dioxolanylmethoxyphenyl-piperazinyl-phenyl-triazolones and antimicrobial compositions
CA1331757C (en) * 1988-02-29 1994-08-30 Janssen Pharmaceutica Naamloze Vennootschap 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols
WO1994020063A2 (en) * 1993-03-04 1994-09-15 Cytoven International N.V. Pharmaceutical tryptophan containing dipeptide compositions and methods of use thereof
US5521186A (en) * 1994-10-27 1996-05-28 Janssen Pharmaceutica N.V. Apolipoprotein-β synthesis inhibitors

Also Published As

Publication number Publication date
ATE198889T1 (de) 2001-02-15
TR199501295A2 (tr) 1996-06-21
CZ286476B6 (en) 2000-04-12
NO971895L (no) 1997-04-24
DK0788496T3 (da) 2001-06-18
NZ295353A (en) 1998-08-26
AU697744C (en) 2002-08-22
PT788496E (pt) 2001-07-31
FI971784A (fi) 1997-04-25
HRP950532A2 (en) 1997-08-31
ES2155535T3 (es) 2001-05-16
DE122007000005I2 (de) 2008-04-24
MX9703074A (es) 1997-07-31
CN1161695A (zh) 1997-10-08
BR9509436A (pt) 1998-01-06
CY2256B1 (en) 2003-07-04
CN1068000C (zh) 2001-07-04
JPH09511759A (ja) 1997-11-25
AU697744B2 (en) 1998-10-15
AP779A (en) 1999-11-03
DE122007000005I1 (de) 2007-04-26
KR100227231B1 (ko) 1999-11-01
GR3035519T3 (en) 2001-06-29
EP0788496A1 (en) 1997-08-13
HUT77360A (hu) 1998-03-30
DE69519995T2 (de) 2001-08-23
DE69519995D1 (en) 2001-03-01
IL115771A (en) 2000-02-29
LU91306I2 (fr) 2007-03-19
CZ119897A3 (cs) 1998-03-18
OA10479A (en) 2002-04-09
RO118715B1 (ro) 2003-09-30
CA2203274A1 (en) 1996-05-09
AU3868095A (en) 1996-05-23
IL115771A0 (en) 1996-01-19
EP0788496B1 (en) 2001-01-24
US5929075A (en) 1999-07-27
JP3025907B2 (ja) 2000-03-27
HU219862B (hu) 2001-08-28
BG63694B1 (bg) 2002-09-30
HRP950532B1 (en) 2001-06-30
AP9700968A0 (en) 1997-04-30
WO1996013499A1 (en) 1996-05-09
NO971895D0 (no) 1997-04-24
CA2203274C (en) 2002-02-19
SK50797A3 (en) 1998-04-08
FI119548B (fi) 2008-12-31
NO311937B1 (no) 2002-02-18
SK281908B6 (sk) 2001-09-11
FI971784A0 (fi) 1997-04-25

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