PE20060102A1 - Pequenas moleculas para el tratamiento de hipercolesterolemia y enfermedades relacionadas - Google Patents

Pequenas moleculas para el tratamiento de hipercolesterolemia y enfermedades relacionadas

Info

Publication number
PE20060102A1
PE20060102A1 PE2005000656A PE2005000656A PE20060102A1 PE 20060102 A1 PE20060102 A1 PE 20060102A1 PE 2005000656 A PE2005000656 A PE 2005000656A PE 2005000656 A PE2005000656 A PE 2005000656A PE 20060102 A1 PE20060102 A1 PE 20060102A1
Authority
PE
Peru
Prior art keywords
amino
acid
guanidin
same
hypercholesterolemia
Prior art date
Application number
PE2005000656A
Other languages
English (en)
Inventor
Jagadish C Sircar
Victor Charles Vassar
Igor Nikoulin
Kashinatham Alisala
Original Assignee
Avanir Pharmaceuticals
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34978959&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20060102(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Avanir Pharmaceuticals filed Critical Avanir Pharmaceuticals
Publication of PE20060102A1 publication Critical patent/PE20060102A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

SE REFIERE A MOLECULAS MEDIADORAS DEL TRANSPORTE INVERSO DE COLESTEROL, QUE COMPRENDEN LA SIGUIENTE ESTRUCTURA: A-B-C, LOS QUE PUEDEN ESTAR EN CUALQUIER ORDEN Y EN DONDE A COMPRENDE UN AMINOACIDO ACIDO O UN BIOISOSTERO DEL MISMO, TAL COMO: -CO2H, CO2-, -SO2H, -SO3H, -PO3H2,-CONR2, -CONR(OH), ENTRE OTROS; B ES AMINOACIDO AROMATICO O LIPOFILICO O UN ANALOGO DEL MISMO, Y C ES UN AMINOACIDO BASICO O UN BIOISOSTERO DEL MISMO, TAL COMO: GUANIDIN, CIANOGUANIDIN, NITROGUANIDIN, GUANIDIN-ANILINA, GUANIDIN-BENZOICO, ENTRE OTROS. ADEMAS UNO DE LOS GRUPOS ALFA-AMINO O ALFA-CARBOXILO FUERON REMOVIDOS DE SUS RESPECTIVOS AMINOACIDOS AMINO O CARBOXILO TERMINALES O SUS ANALOGOS. SON COMPUESTOS PREFERIDOS: ACIDO 4-(1-(4-GUANIDINBUTILCARBAMOIL)-2-(1-METIL-1H-INDOL-3-IL) ETILCARBAMOIL) BUTANOICO, (R)-{METIL ESTER DEL ACIDO N-[1-(4-AMINO-FENILCARBAMOIL)-2-FENIL-ETIL]-TER-FTALAMICO}, (S)-{N-[1-(4-AMINO-FENILCARBAMOIL)-2-FENIL-ETIL]-4-(1H-TETRAZOL-5-IL)BENZAMIDA}, ENTRE OTROS. ESTAS MOLECULAS IMITAN LA ACTIVIDAD DE LA ApoA-I, Y SON UTILES PARA EL TRATAMIENTO Y/O LA PREVENCION DE HIPERCOLESTEROLEMIA, ARTEROSCLEROSIS ENFERMEDADES CARDIOVASCULARES ASOCIADAS
PE2005000656A 2004-06-09 2005-06-09 Pequenas moleculas para el tratamiento de hipercolesterolemia y enfermedades relacionadas PE20060102A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57822804P 2004-06-09 2004-06-09

Publications (1)

Publication Number Publication Date
PE20060102A1 true PE20060102A1 (es) 2006-02-09

Family

ID=34978959

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000656A PE20060102A1 (es) 2004-06-09 2005-06-09 Pequenas moleculas para el tratamiento de hipercolesterolemia y enfermedades relacionadas

Country Status (17)

Country Link
US (1) US20050277690A1 (es)
EP (1) EP1753733A1 (es)
JP (1) JP2008502737A (es)
KR (1) KR20070043711A (es)
CN (1) CN1964955A (es)
AR (1) AR049217A1 (es)
AU (1) AU2005255012A1 (es)
BR (1) BRPI0511871A (es)
CA (1) CA2568539A1 (es)
IL (1) IL179209A0 (es)
MX (1) MXJL06000070A (es)
NO (1) NO20070141L (es)
PE (1) PE20060102A1 (es)
RU (1) RU2006146479A (es)
TW (1) TW200603794A (es)
UY (1) UY28951A1 (es)
WO (1) WO2005123700A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1753782A1 (en) * 2004-06-09 2007-02-21 Avanir Pharmaceuticals Mediators of reverse cholesterol transport for the treatment of hypercholesterolemia
CN106916086A (zh) * 2015-12-28 2017-07-04 深圳翰宇药业股份有限公司 一种对硝基苯胺修饰多肽c端的固相合成方法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3930024A (en) * 1969-09-02 1975-12-30 Parke Davis & Co Pharmaceutical compositions and methods
US3773946A (en) * 1969-09-02 1973-11-20 Parke Davis & Co Triglyceride-lowering compositions and methods
US4448785A (en) * 1978-01-09 1984-05-15 Sandoz, Inc. N-Unsaturated fatty acid amides of tryptophan ester homologues and anti-cholesteric use thereof
JPS5522636A (en) * 1978-08-04 1980-02-18 Takeda Chem Ind Ltd Thiazoliding derivative
IL64542A0 (en) * 1981-12-15 1982-03-31 Yissum Res Dev Co Long-chain alpha,omega-dicarboxylic acids and derivatives thereof and pharmaceutical compositions containing them
JPS60136512A (ja) * 1983-12-26 1985-07-20 Eisai Co Ltd 脂質代謝改善剤
US4643988A (en) * 1984-05-15 1987-02-17 Research Corporation Amphipathic peptides
DE3423166A1 (de) * 1984-06-22 1986-01-02 Epis S.A., Zug Alpha-, omega-dicarbonsaeuren, verfahren zu ihrer herstellung und arzneimittel, die diese verbindungen enthalten
US5648387A (en) * 1995-03-24 1997-07-15 Warner-Lambert Company Carboxyalkylethers, formulations, and treatment of vascular diseases
JPH10316641A (ja) * 1997-03-14 1998-12-02 Sankyo Co Ltd カルボン酸誘導体
AU8334298A (en) * 1997-07-15 1999-02-10 Novo Nordisk A/S Nociceptin analogues
US6004925A (en) * 1997-09-29 1999-12-21 J. L. Dasseux Apolipoprotein A-I agonists and their use to treat dyslipidemic disorders
IL145712A0 (en) * 1999-04-01 2002-07-25 Esperion Therapeutics Inc Ether compounds, compositions, and uses thereof
US7148197B2 (en) * 2000-08-24 2006-12-12 The Regents Of The University Of California Orally administered small peptides synergize statin activity
US6664230B1 (en) * 2000-08-24 2003-12-16 The Regents Of The University Of California Orally administered peptides to ameliorate atherosclerosis
FR2820435B1 (fr) * 2001-02-05 2004-02-27 Genfit S A Procedes d'identification de composes modulant le transport inverse du cholesterol
US7429593B2 (en) * 2001-09-14 2008-09-30 Shionogi & Co., Ltd. Utilities of amide compounds
US20060166891A1 (en) * 2003-04-22 2006-07-27 Sircar Jagadish C Mediators of reverse cholesterol transport for the treatment of hypercholesterolemia

Also Published As

Publication number Publication date
KR20070043711A (ko) 2007-04-25
EP1753733A1 (en) 2007-02-21
RU2006146479A (ru) 2008-07-20
NO20070141L (no) 2007-03-02
IL179209A0 (en) 2007-03-08
JP2008502737A (ja) 2008-01-31
WO2005123700A1 (en) 2005-12-29
TW200603794A (en) 2006-02-01
CA2568539A1 (en) 2005-12-29
AR049217A1 (es) 2006-07-05
CN1964955A (zh) 2007-05-16
UY28951A1 (es) 2006-01-31
AU2005255012A1 (en) 2005-12-29
MXJL06000070A (es) 2007-04-10
BRPI0511871A (pt) 2008-01-15
US20050277690A1 (en) 2005-12-15

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