[go: up one dir, main page]

BR9807222A - Inibidor da atividade de cetp. - Google Patents

Inibidor da atividade de cetp.

Info

Publication number
BR9807222A
BR9807222A BR9807222-6A BR9807222A BR9807222A BR 9807222 A BR9807222 A BR 9807222A BR 9807222 A BR9807222 A BR 9807222A BR 9807222 A BR9807222 A BR 9807222A
Authority
BR
Brazil
Prior art keywords
group
substituted
unsubstituted
cetp activity
inhibitor
Prior art date
Application number
BR9807222-6A
Other languages
English (en)
Other versions
BRPI9807222B1 (pt
BRPI9807222B8 (pt
Inventor
Hisashi Shinkai
Kimiya Maeda
Hiroshi Okamoto
Original Assignee
Japan Tobacco Inc
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 Japan Tobacco Inc filed Critical Japan Tobacco Inc
Publication of BR9807222A publication Critical patent/BR9807222A/pt
Publication of BRPI9807222B1 publication Critical patent/BRPI9807222B1/pt
Publication of BRPI9807222B8 publication Critical patent/BRPI9807222B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having 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
    • A61K31/33—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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • C07C323/40—Y being a hydrogen or a carbon atom
    • 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
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C07C323/41—Y being a hydrogen or an acyclic carbon atom
    • 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
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C07C323/42—Y being a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C329/00—Thiocarbonic acids; Halides, esters or anhydrides thereof
    • C07C329/02—Monothiocarbonic acids; Derivatives thereof
    • C07C329/04—Esters of monothiocarbonic acids
    • C07C329/10—Esters of monothiocarbonic acids having sulfur atoms of thiocarbonic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C329/00—Thiocarbonic acids; Halides, esters or anhydrides thereof
    • C07C329/12—Dithiocarbonic acids; Derivatives thereof
    • C07C329/14—Esters of dithiocarbonic acids
    • C07C329/20—Esters of dithiocarbonic acids having sulfur atoms of dithiocarbonic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C333/00—Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C333/02—Monothiocarbamic acids; Derivatives thereof
    • C07C333/04—Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C333/00—Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C333/02—Monothiocarbamic acids; Derivatives thereof
    • C07C333/08—Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C333/00—Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C333/02—Monothiocarbamic acids; Derivatives thereof
    • C07C333/10—Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups being part of any of the groups, X being a hetero atom, Y being any atom, e.g., N-acyl-thiocarbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon 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
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/22—All rings being cycloaliphatic the ring system containing eight carbon atoms, e.g. pentalene
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/26—All rings being cycloaliphatic the ring system containing ten carbon atoms
    • C07C2602/28—Hydrogenated naphthalenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74—Adamantanes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Cosmetics (AREA)

Abstract

Patente de Invenção:<B>"INIBIDOR DA ATIVIDADE DE CETP"<D>. A presente invenção fornece um inibidor da atividade de CETP compreendendo como ingrediente ativo um composto representado pela fórmula (I): onde R representa um grupo alquila de cadeia reta ou ramificada; um grupo alquenila de cadeia reta ou ramificada; um grupo haloalquila inferior; um grupo cicloalquila substituída ou não substituída; um grupo cicloalquenila substituída ou não substituída; um grupo cicloalquilalquila substituída ou não substituída; um grupo arila substituída ou não substituída; ou um grupo heterocíclico substituída ou não substituído, X~ 1~, X~ 2~, X~ 3~e X~ 4~ podem ser iguais ou diferentes e cada uma representa um átomo de hidrogênio, um átomo de halogênio, um grupo alquila inferior, um grupo haloalquila inferior; um grupo alcóxi inferior; um grupo ciano; um grupo nitro; um grupo acila; ou um grupo arial, Y representa -CO- ou -SO~ 2~-, e Z representa um átomo de hidrogênio ou um grupo protetor de mercapto, ou um composto pró-droga, um sal ou hidrato ou solvato farmaceuticamente aceitável do mesmo. Os compostos representados pela fórmula (I) podem aumentar HDL e ao mesmo tempo diminuir LDL por meio de inibição seletiva da atividade de CETP e, portanto, acredita-se ser útil como um tipo novo de agente preventivo ou terapêutico para ateroesclerose ou hiperlipidemia.
BRPI9807222A 1997-02-12 1998-02-10 compostos inibidores da atividade de cetp, seus usos e composições farmacêuticas BRPI9807222B8 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP4483697 1997-02-12
JP16508597 1997-06-05
JP10026688A JP2894445B2 (ja) 1997-02-12 1998-01-23 Ｃｅｔｐ活性阻害剤として有効な化合物
PCT/JP1998/000542 WO1998035937A1 (en) 1997-02-12 1998-02-10 Cetp activity inhibitors

Publications (3)

Publication Number Publication Date
BR9807222A true BR9807222A (pt) 2000-05-23
BRPI9807222B1 BRPI9807222B1 (pt) 2016-08-02
BRPI9807222B8 BRPI9807222B8 (pt) 2021-05-25

Family

ID=27285497

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI9807222A BRPI9807222B8 (pt) 1997-02-12 1998-02-10 compostos inibidores da atividade de cetp, seus usos e composições farmacêuticas

Country Status (24)

Country Link
US (6) US6426365B1 (pt)
EP (3) EP2292596A3 (pt)
JP (1) JP2894445B2 (pt)
KR (1) KR100324183B1 (pt)
CN (1) CN100384821C (pt)
AT (1) ATE338029T1 (pt)
AU (1) AU728979B2 (pt)
BR (1) BRPI9807222B8 (pt)
CA (1) CA2280708C (pt)
CY (1) CY2587B2 (pt)
CZ (1) CZ302069B6 (pt)
DE (1) DE69835760T2 (pt)
DK (1) DK1020439T3 (pt)
ES (1) ES2270504T3 (pt)
HU (1) HU227763B1 (pt)
ID (1) ID22667A (pt)
IL (2) IL131250A (pt)
NO (1) NO314228B1 (pt)
NZ (1) NZ337122A (pt)
PT (1) PT1020439E (pt)
RU (1) RU2188631C2 (pt)
SK (1) SK282973B6 (pt)
TW (1) TW577865B (pt)
WO (1) WO1998035937A1 (pt)

Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4861580A (en) * 1985-10-15 1989-08-29 The Liposome Company, Inc. Composition using salt form of organic acid derivative of alpha-tocopheral
US6642268B2 (en) 1994-09-13 2003-11-04 G.D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors
US6262277B1 (en) 1994-09-13 2001-07-17 G.D. Searle And Company Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
JP2894445B2 (ja) * 1997-02-12 1999-05-24 日本たばこ産業株式会社 Ｃｅｔｐ活性阻害剤として有効な化合物
US6605624B1 (en) 1998-02-13 2003-08-12 Pharmacia Corporation Substituted pyridines useful for inhibiting cholesteryl ester transfer protein activity
PT1140184E (pt) 1998-12-23 2003-10-31 Searle Llc Combinacoes de inibidores de proteina de transferencia de ester de colesterilo com derivados de acido nicotinico para indicacoes cardiovasculares
JP3498624B2 (ja) * 1999-03-31 2004-02-16 株式会社デンソー レーダ装置
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
US20040229781A1 (en) * 2000-05-10 2004-11-18 Marks Andrew Robert Compounds and methods for treating and preventing exercise-induced cardiac arrhythmias
US7718644B2 (en) 2004-01-22 2010-05-18 The Trustees Of Columbia University In The City Of New York Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof
US6489125B1 (en) * 2000-05-10 2002-12-03 The Trustees Of Columbia University In The City Of New York Methods for identifying chemical compounds that inhibit dissociation of FKBP12.6 binding protein from type 2 ryanodine receptor
US7879840B2 (en) 2005-08-25 2011-02-01 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the RyR receptors
US20040048780A1 (en) * 2000-05-10 2004-03-11 The Trustees Of Columbia University In The City Of New York Method for treating and preventing cardiac arrhythmia
US20060293266A1 (en) * 2000-05-10 2006-12-28 The Trustees Of Columbia Phosphodiesterase 4D in the ryanodine receptor complex protects against heart failure
US8022058B2 (en) 2000-05-10 2011-09-20 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the RyR receptors
US7393652B2 (en) 2000-05-10 2008-07-01 The Trustees Of Columbia University In The City Of New York Methods for identifying a chemical compound that directly enhances binding of FKBP12.6 to PKA-phosphorylated type 2 ryanodine receptor (RyR2)
CA2407964A1 (en) 2000-05-19 2001-11-29 Alcon, Inc. Disulfide derivatives useful for treating allergic diseases
PL365459A1 (en) * 2000-05-19 2005-01-10 Alcon, Inc. Aniline disulfide derivatives for treating allergic diseases
PL363102A1 (en) 2000-05-19 2004-11-15 Alcon Inc. Compositions containing a benzamide disulfide derivative for treating allergic diseases
JP2002069033A (ja) * 2000-06-16 2002-03-08 Japan Tobacco Inc １−置換−シクロヘキサンカルボニルハライド化合物の製造方法
US7115279B2 (en) 2000-08-03 2006-10-03 Curatolo William J Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors
EP1362846A4 (en) * 2001-01-26 2006-10-04 Takeda Pharmaceutical AMINOETHANOL DERIVATIVES
EE200400024A (et) 2001-06-21 2004-06-15 Pfizer Products Inc. Kolesterüülestri ülekandevalgu inhibiitorite iseemulgeeruvad formulatsioonid
OA12625A (en) 2001-06-22 2006-06-12 Pfizer Prod Inc Pharmaceutical compositions of adsorbates of amorphous drug.
MXPA03011784A (es) 2001-06-22 2004-04-02 Pfizer Prod Inc Composiciones farmaceuticas de dispersiones de farmacos y polimeros neutros.
EP1269994A3 (en) 2001-06-22 2003-02-12 Pfizer Products Inc. Pharmaceutical compositions comprising drug and concentration-enhancing polymers
EP1269982A1 (en) * 2001-06-30 2003-01-02 Givaudan SA Fragrance and flavour compositions
US7202247B2 (en) 2001-12-19 2007-04-10 Atherogenics, Inc. 1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders
WO2003053368A2 (en) 2001-12-19 2003-07-03 Atherogenics, Inc. Chalcone derivatives and their use to treat diseases
US6852753B2 (en) 2002-01-17 2005-02-08 Pharmacia Corporation Alkyl/aryl hydroxy or keto thiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
AR038375A1 (es) 2002-02-01 2005-01-12 Pfizer Prod Inc Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo
TW200307539A (en) * 2002-02-01 2003-12-16 Bristol Myers Squibb Co Cycloalkyl inhibitors of potassium channel function
EP1469832B2 (en) 2002-02-01 2016-10-26 Bend Research, Inc. Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials
US20050080024A1 (en) * 2002-08-15 2005-04-14 Joseph Tucker Nitric oxide donating derivatives for the treatment of cardiovascular disorders
US20050080021A1 (en) * 2002-08-15 2005-04-14 Joseph Tucker Nitric oxide donating derivatives of stilbenes, polyphenols and flavonoids for the treatment of cardiovascular disorders
EP1533292B1 (en) * 2002-08-30 2007-02-14 Japan Tobacco Inc. Dibenzylamine compound and medicinal use thereof
US7544678B2 (en) 2002-11-05 2009-06-09 The Trustees Of Columbia University In The City Of New York Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2)
MXPA05005813A (es) 2002-12-20 2005-12-12 Pfizer Prod Inc Formas de dosificacion que comprenden un inhibidor de la cetp y un inhibidor de la hmg-coa reductasa.
AU2004220548A1 (en) 2003-03-07 2004-09-23 The Trustees Of Columbia University, In The City Of New York Type 1 ryanodine receptor-based methods
AU2004222436A1 (en) * 2003-03-17 2004-09-30 Japan Tobacco Inc. Method for increasing the oral bioavailability of S-(2-(((1- (2-ethylbutyl) cyclohexyl)carbonyl) amino) phenyl)-2-methylpropanethioate
NZ542852A (en) 2003-03-17 2008-09-26 Japan Tobacco Inc Pharmaceutical compositions of CETP inhibitors
CN101036636A (zh) * 2003-03-17 2007-09-19 日本烟草产业株式会社 提高s－[2－([[1－(2－乙基丁基)环己基]羰基]氨基)苯基]－2－甲基丙硫代酸酯口服生物利用度的方法
TWI494102B (zh) * 2003-05-02 2015-08-01 Japan Tobacco Inc 包含ｓ-〔２（〔〔１-（２-乙基丁基）環己基〕羰基〕胺基）苯基〕２-甲基丙烷硫酯及ｈｍｇ輔酶ａ還原酶抑制劑之組合
OA13174A (en) * 2003-05-30 2006-12-13 Ranbaxy Lab Ltd Substituted pyrrole derivatives and their use as HMG-Co inhibitors.
CL2004001884A1 (es) 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
MXPA06001417A (es) 2003-08-04 2006-05-15 Pfizer Prod Inc Composiciones farmaceuticas de adsorbatos de farmacos amorfos y materiales que forman microfases lipofilas.
RU2318504C2 (ru) * 2003-08-08 2008-03-10 Джапан Тобакко Инк. Фармацевтические композиции сетр-ингибиторов
CN101342162A (zh) * 2003-09-26 2009-01-14 日本烟草产业株式会社 抑制残余脂蛋白产生的方法
US8710045B2 (en) 2004-01-22 2014-04-29 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the ryanodine receptors
TW200606157A (en) * 2004-07-02 2006-02-16 Sankyo Co Suppressant of production of tissue factor
AU2005297984B2 (en) 2004-10-27 2009-11-12 Daiichi Sankyo Company, Limited Benzene compound having 2 or more substituents
GB0425661D0 (en) * 2004-11-23 2004-12-22 Givaudan Sa Organic compounds
WO2006082518A1 (en) 2005-02-03 2006-08-10 Pfizer Products Inc. Pharmaceutical compositions with enhanced performance
WO2006098394A1 (ja) * 2005-03-14 2006-09-21 Japan Tobacco Inc. 脂質吸収抑制方法および脂質吸収抑制剤
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
US7704990B2 (en) 2005-08-25 2010-04-27 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the RyR receptors
WO2007047591A2 (en) * 2005-10-19 2007-04-26 Merck & Co., Inc. Cetp inhibitors
WO2007048027A2 (en) 2005-10-21 2007-04-26 Novartis Ag Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent
US7435849B2 (en) 2005-10-31 2008-10-14 Hoffmann-La Roche Inc. Process for the production of acid chlorides
WO2007054896A1 (en) * 2005-11-08 2007-05-18 Ranbaxy Laboratories Limited Process for (3r, 5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt
US8383660B2 (en) * 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
US7919506B2 (en) * 2006-03-10 2011-04-05 Pfizer Inc. Dibenzyl amine compounds and derivatives
WO2008020314A2 (en) * 2006-03-14 2008-02-21 Ranbaxy Laboratories Limited Statin stabilizing dosage formulations
CN101096363B (zh) * 2006-06-27 2011-05-11 中国人民解放军军事医学科学院毒物药物研究所 2,4,5-三取代噻唑类化合物、其制备方法、药物组合物及其制药用途
WO2008010087A2 (en) * 2006-07-14 2008-01-24 Ranbaxy Laboratories Limited Polymorphic forms of an hmg-coa reductase inhibitor and uses thereof
US7750019B2 (en) 2006-08-11 2010-07-06 Kowa Company, Ltd. Pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same
EP1935867A1 (en) * 2006-12-20 2008-06-25 F. Hoffmann-La Roche Ag Process for preparing 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
US7790737B2 (en) 2007-03-13 2010-09-07 Kowa Company, Ltd. Substituted pyrimidine compounds and their utility as CETP inhibitors
WO2008129951A1 (ja) 2007-04-13 2008-10-30 Kowa Company, Ltd. 新規なジベンジルアミン構造を有するピリミジン化合物及びこれを含有する医薬
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
CA2684067A1 (en) * 2007-04-25 2008-11-06 F. Hoffmann-La Roche Ag Novel process for the preparation of acid chlorides
CA2717959C (en) * 2008-04-04 2016-03-22 F. Hoffmann-La Roche Ag New process for the preparation of cyclohexanecarboxylic acid derivatives via the corresponding cyclohexanecarboxamide derivative
BRPI0909813B1 (pt) * 2008-04-04 2018-01-02 F. Hoffmann-La Roche Ag "processos para preparação de derivados de ácido ciclo-hexanocarboxílico, e intermediário"
CA2726931C (en) * 2008-06-17 2016-03-22 F.Hoffmann-La Roche Ag 1-(2-ethyl-butyl) -cyclohexanecarboxylic acid ester as an intermediate in the preparation of pharmaceutically active amides
EP2379562A1 (en) 2008-12-16 2011-10-26 Schering Corporation Bicyclic pyranone derivatives as nicotinic acid receptor agonists
US20110245209A1 (en) 2008-12-16 2011-10-06 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
US8178583B2 (en) * 2008-12-19 2012-05-15 Hoffmann-La Roche Inc. Compounds
US20110004011A1 (en) * 2009-07-01 2011-01-06 Declan Costello Novel process
NZ598685A (en) 2009-09-11 2013-05-31 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
WO2011101424A1 (en) 2010-02-19 2011-08-25 Boehringer Ingelheim International Gmbh Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
DK2545047T3 (da) 2010-03-10 2014-07-28 Probiodrug Ag Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
EP2635263B1 (en) 2010-11-04 2015-09-23 F.Hoffmann-La Roche Ag A composition comprising s-[2-([[1-(2-ethylbutyl)-cyclohexyl]-carbonyl]amino)phenyl]2-methylpropanethioate and croscarmellose sodium
MX2013006031A (es) 2010-12-08 2013-07-15 Hoffmann La Roche Formulacion liposomal de dalcetrapib.
ES2705496T3 (es) * 2010-12-16 2019-03-25 Hoffmann La Roche Procedimiento para la preparación de derivados de tiol aromáticos por hidrogenación de disulfuros
EP2675434A1 (en) 2011-02-17 2013-12-25 F.Hoffmann-La Roche Ag A process for controlled crystallization of an active pharmaceutical ingredient from supercooled liquid state by hot melt extrusion
US20130053404A1 (en) 2011-02-17 2013-02-28 Boehringer Ingelheim International Gmbh Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
MX342104B (es) 2011-04-12 2016-09-13 Chong Kun Dang Pharmaceutical Corp Derivados de cicloalquenil arilo para inhibidor de cetp.
US8975438B2 (en) 2011-07-13 2015-03-10 Hoffmann-La Roche Inc. Process for the preparation of cyclohexanecarboxylic acid derivatives
WO2013024130A1 (en) 2011-08-17 2013-02-21 Boehringer Ingelheim International Gmbh Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation
US20140303198A1 (en) 2011-11-29 2014-10-09 Kowa Company, Ltd. Agent for inhibiting expression of npc1l1 and/or lipg mrna and agent for preventing and/or treating obesity
JP2015515498A (ja) 2012-04-30 2015-05-28 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規製剤
MX347400B (es) 2012-06-29 2017-04-18 Univ Nac Autónoma De México Vacuna de aplicacion nasal contra el desarrollo de la enfermedad aterosclerotica y el higado graso.
CN105143193B (zh) 2013-01-31 2017-12-15 株式会社钟根堂 作为cetp抑制剂的联芳基或杂环联芳基取代的环己烯衍生化合物
US9119732B2 (en) 2013-03-15 2015-09-01 Orthocision, Inc. Method and implant system for sacroiliac joint fixation and fusion
HUE039973T2 (hu) 2013-03-27 2019-02-28 Hoffmann La Roche Genetikai markerek a terápiára való válaszadó képesség elõrejelzéséhez
EP3524238A1 (en) * 2013-12-19 2019-08-14 F. Hoffmann-La Roche AG Cetp modulator for use in the treatment of eye disease
EP3174995B1 (en) 2014-07-30 2020-08-19 F.Hoffmann-La Roche Ag Genetic markers for predicting responsiveness to therapy with hdl-raising or hdl mimicking agent
US12150975B2 (en) 2016-07-27 2024-11-26 Hartis-Pharma Sa Therapeutic combinations to treat red blood cell disorders
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2596755A (en) * 1948-01-13 1952-05-13 Eastman Kodak Co Aromatic color couplers containing mercaptan and hydroxyl groups
US2787621A (en) * 1953-10-22 1957-04-02 American Cyanamid Co Metal salts of acylated aminothiophenols as catalytic plasticizers for rubber
US3072707A (en) * 1956-06-12 1963-01-08 Goodyear Tire & Rubber Aryl disulfides
US3260695A (en) * 1962-06-04 1966-07-12 Union Carbide Canada Ltd Stress crack resistant polyethylene composition containing zinc-2-benzamidothiophenate
NL300271A (pt) * 1962-11-09
US3576830A (en) 1966-08-12 1971-04-27 Sumitomo Chemical Co Amides containing sulfur
US3920444A (en) * 1970-12-21 1975-11-18 Minnesota Mining & Mfg Method comprising the use of N-substituted perfluoroalkyanesulfonamides as herbicidal and plant growth modifying agents, and composition
JPS4735786U (pt) 1971-05-10 1972-12-20
US4033756A (en) * 1971-09-17 1977-07-05 Gulf Research & Development Company Dichloroacetamide treated rice seeds
US3856840A (en) * 1972-12-11 1974-12-24 Rohm & Haas Organotin heterocyclic compounds
US4038300A (en) * 1974-08-23 1977-07-26 Belmares Sarabia Hector Polymerizable ethylenically unsaturated n-substituted 2,2-dihydro carbyl-2,1,3-benzostanna-thiazolines
US4157444A (en) * 1978-03-13 1979-06-05 American Cyanamid Company 10-(Piperazinyl)thieno[3,4-b][1,5]benzoxazepines and 10-(piperazinyl)thieno[3,4-b][1,5]benzothiazepines
US4268301A (en) * 1978-04-17 1981-05-19 Sumitomo Chemical Company, Limited 1,4-Benzothiazines
JPS60119445A (ja) 1983-11-30 1985-06-26 Shimadzu Corp 化学発光式分析計
JPS60119443A (ja) 1983-11-30 1985-06-26 Shimadzu Corp 光吸収式ガス分析計
DE3623422A1 (de) * 1986-07-11 1988-01-14 Basf Ag Verfahren zur herstellung von carbonsaeurehalogeniden
US4740438A (en) 1986-12-10 1988-04-26 Eastman Kodak Company Organic disulfides as image dye stabilizers
US4853319A (en) 1986-12-22 1989-08-01 Eastman Kodak Company Photographic silver halide element and process
JPS6486821A (en) 1987-09-29 1989-03-31 Daiden Co Ltd Root culture in flooded, level lowered and moistened conditions
JPH01117730A (ja) 1987-10-29 1989-05-10 Daiden Kk 水気耕栽培方法及びそれに用いる組合わせ容器
JPH01278543A (ja) 1988-04-30 1989-11-08 Sanshin Chem Ind Co Ltd ゴム組成物
JPH01321432A (ja) 1988-06-22 1989-12-27 Konica Corp ハロゲン化銀写真感光材料
JPH0223338A (ja) 1988-07-12 1990-01-25 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
JPH02284146A (ja) 1989-04-25 1990-11-21 Mitsubishi Paper Mills Ltd 平版印刷版用処理液組成物
US5118583A (en) 1988-10-12 1992-06-02 Mitsubishi Paper Mills Limited Processing composition for printing plate
DE3835198A1 (de) 1988-10-15 1990-04-19 Bayer Ag Verfahren zur herstellung von kautschukvulkanisaten mit verringerten hystereseverlusten und formkoerper aus diesen vulkanisaten
JPH03226750A (ja) 1990-01-31 1991-10-07 Konica Corp ハロゲン化銀カラー写真感光材料
FR2665450B1 (fr) 1990-08-01 1994-04-08 Rhone Poulenc Chimie Procede de preparation de dispersions aqueuses de copolymeres.
GB9017711D0 (en) * 1990-08-13 1990-09-26 May & Baker Ltd New compositions of matter
GB9017710D0 (en) * 1990-08-13 1990-09-26 May & Baker Ltd New compositions of matter
US5447830A (en) * 1991-04-23 1995-09-05 Eastman Kodak Company 3-anilino pyrazolone magenta couplers and process
US5217859A (en) 1992-04-16 1993-06-08 Eastman Kodak Company Aqueous, solid particle dispersions of dichalcogenides for photographic emulsions and coatings
US5219721A (en) 1992-04-16 1993-06-15 Eastman Kodak Company Silver halide photographic emulsions sensitized in the presence of organic dichalcogenides
EP0594897B1 (en) * 1992-10-30 1998-03-18 Agfa-Gevaert N.V. A photographic material containing a mixture of silver halide emulsions
US5350667A (en) 1993-06-17 1994-09-27 Eastman Kodak Company Photographic elements containing magenta couplers and process for using same
IL110151A (en) 1993-06-30 1998-10-30 Sankyo Co Amide derivatives and pharmaceutical compositions containing them
HUT73813A (en) * 1993-06-30 1996-09-30 Wellcome Found Anti-athero-sclerotic diaryl compounds, process to prepare them and pharmaceutical compositions contg. them
US5446207A (en) 1993-09-01 1995-08-29 Harbor Branch Oceanographic Institution, Inc. Anti-dyslipidemic agents
US5459154A (en) * 1993-11-08 1995-10-17 American Home Products Corporation N-hydroxyureas as 5-lipoxygenase inhibitors and inhibitors of oxidative modification of low density lipoprotein
US5405969A (en) 1993-12-10 1995-04-11 Eastman Kodak Company Manufacture of thioether compounds
JP3304189B2 (ja) 1994-03-18 2002-07-22 マツダ株式会社 加硫スクラップゴムを含有する成形用ゴム組成物及びその製造方法
US5654134A (en) 1994-05-18 1997-08-05 Fuji Photo Film Co., Ltd. Silver halide emulsion
DE4428457C1 (de) 1994-08-11 1995-10-05 Bayer Ag Geformte, paraffinhaltige Mastiziermittel
US6001555A (en) 1994-09-23 1999-12-14 The United States Of America As Represented By The Department Of Health And Human Services Method for identifying and using compounds that inactivate HIV-1 and other retroviruses by attacking highly conserved zinc fingers in the viral nucleocapsid protein
JP3485210B2 (ja) 1994-10-19 2004-01-13 富士写真フイルム株式会社 ハロゲン化銀乳剤
JPH08130660A (ja) 1994-10-28 1996-05-21 Victor Co Of Japan Ltd フォーカス電圧供給回路
EP0720983B1 (en) 1994-12-26 2001-03-14 Nisshin Flour Milling Co., Ltd. Diphenyl disulfide compounds
JPH08253454A (ja) 1994-12-26 1996-10-01 Nisshin Flour Milling Co Ltd ジフェニルジスルフィド化合物
JP3226750B2 (ja) 1995-03-03 2001-11-05 大和コンピューターサービス株式会社 検査システム
DE19517448A1 (de) * 1995-05-12 1996-11-14 Thomae Gmbh Dr K Neue Benzothiazole und Benzoxazole, diese Verbindungen enthaltende Arzneimittel und deren Verwendung sowie Verfahren zu ihrer Herstellung
DE19610932A1 (de) 1996-03-20 1997-09-25 Bayer Ag 2-Aryl-substituierte Pyridine
JP2894445B2 (ja) 1997-02-12 1999-05-24 日本たばこ産業株式会社 Ｃｅｔｐ活性阻害剤として有効な化合物
AU9297798A (en) * 1997-09-16 1999-04-05 G.D. Searle & Co. Substituted 1,2,4-triazoles useful for inhibiting cholesteryl ester transfer protein activity
US6147089A (en) * 1998-09-17 2000-11-14 Pfizer Inc. Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines
JP4511132B2 (ja) 2003-02-07 2010-07-28 志良 平賀 ブレーカー遮断装置

Also Published As

Publication number Publication date
EP1020439B1 (en) 2006-08-30
JPH1149743A (ja) 1999-02-23
SK282973B6 (sk) 2003-01-09
NO993869D0 (no) 1999-08-11
NO993869L (no) 1999-09-23
PT1020439E (pt) 2006-10-31
NO314228B1 (no) 2003-02-17
HUP0002483A2 (hu) 2001-05-28
BRPI9807222B1 (pt) 2016-08-02
JP2894445B2 (ja) 1999-05-24
IL131250A0 (en) 2001-01-28
AU5781898A (en) 1998-09-08
CZ278899A3 (cs) 2000-02-16
US20100197736A1 (en) 2010-08-05
TW577865B (en) 2004-03-01
NZ337122A (en) 2001-02-23
IL164569A (en) 2010-11-30
HK1029784A1 (en) 2001-04-12
US20040229957A1 (en) 2004-11-18
KR20000070982A (ko) 2000-11-25
EP1710231A1 (en) 2006-10-11
CZ302069B6 (cs) 2010-09-29
BRPI9807222B8 (pt) 2021-05-25
WO1998035937A1 (en) 1998-08-20
US6753346B2 (en) 2004-06-22
KR100324183B1 (ko) 2002-02-16
AU728979B2 (en) 2001-01-25
US7579379B2 (en) 2009-08-25
EP2292596A3 (en) 2011-06-15
CA2280708A1 (en) 1998-08-20
EP1020439A4 (en) 2004-12-15
ATE338029T1 (de) 2006-09-15
US20080027109A1 (en) 2008-01-31
US9000045B2 (en) 2015-04-07
IL131250A (en) 2004-12-15
RU2188631C2 (ru) 2002-09-10
US20030092708A1 (en) 2003-05-15
US20130053417A1 (en) 2013-02-28
DK1020439T3 (da) 2006-11-27
CA2280708C (en) 2004-09-14
DE69835760D1 (de) 2006-10-12
HU227763B1 (en) 2012-02-28
HUP0002483A3 (en) 2001-12-28
SK109599A3 (en) 2000-05-16
CY2587B2 (en) 2009-11-04
CN1252053A (zh) 2000-05-03
ES2270504T3 (es) 2007-04-01
EP2292596A2 (en) 2011-03-09
DE69835760T2 (de) 2007-09-13
US6426365B1 (en) 2002-07-30
ID22667A (id) 1999-12-02
US7271196B2 (en) 2007-09-18
IL164569A0 (en) 2005-12-18
EP1020439A1 (en) 2000-07-19
CN100384821C (zh) 2008-04-30

Similar Documents

Publication Publication Date Title
BR9807222A (pt) Inibidor da atividade de cetp.
TW200420542A (en) A compound having TGF β inhibition activity and a medicinal composition containing the same
ES2191484T3 (es) Compuestos heterociclicos como inhibidores de enzimas de rotamasa.
DK1201678T3 (da) Hidtil ukendte bicyklonukleosidanaloger
BR0012697A (pt) Inibidores da diferenciação de th2
BRPI0418082B8 (pt) derivados de tiazol úteis como antagonistas de receptor de adenosina a2a
PT937722E (pt) Derivados de benzimidazole como inibidores de ciclooxigenase-2
BR9815171A (pt) Composto inibidor de pde iv aplicável no tratamento de doenças, particularmente de asma, em mamìferos e método para tratar um paciente sofrendo estados doentios.
BRPI0509307A (pt) compostos de alfa aril ou heteroaril metil beta piperidino propanamida como antagonistas do receptor orl1
BR0312999A (pt) Compostos, composições farmacêticas, método para aumentar a cognição, de tratamento, de inibição da atividade de enzima pde4 em um paciente
BR9809062A (pt) Inibidores da metaloproteinase, composições farmacêuticas comtendo os mesmos e seus usos farmacêuticos
ES8801245A1 (es) Un procedimiento para preparar derivados de piperidina
BR9914355A (pt) Derivados de mononitrato de isosorbida e sua utilização como agentes vasodilatadores com tolerância reduzida
BR0014615A (pt) Derivado de ácido fosfÈnico que apresenta atividade inibidora contra carboxipeptidase b
EP1252890A4 (en) MEDICINAL AND PREVENTIVE AGENTS FOR DIGESTIVE DISEASES CONTAINING DIAMINOTRIFLUOROMETHYLPYRIDINE COMPOUNDS
DE60309349D1 (de) Propanamine derivate als serotonin und norepinephrin reuptake-inhibitoren
AR011571A1 (es) Un derivado de naftaleno, su uso, una composicion farmaceutica que lo comprende y un procedimiento para su preparacion
BR9914438A (pt) Processo aperfeiçoado para a preparação de novos agentes anti-diabéticos
ATE229538T1 (de) 22r-hydroxycholesta-8,14-diene derivate zur hemmung der meiose
NO20012443L (no) Benzoksazolderivater og legemidler inneholdende disse som aktiv bestanddel
KR900014344A (ko) 아미노벤젠술폰산 유도체
TR199901932T2 (xx) CETP aktivitesi inhibitörleri.
BR9712763A (pt) Derivados de benzenosulfonamida e medicamentos que contêm tais derivados
BR9709074A (pt) Derivados de polihidroxifenol agentes de prevencão e terapéuticos para doencas ósseas e de cartilagem contendo os mesmos
AR015707A1 (es) UN COMPUESTO INHIBIDOR DE LA ACTIVIDAD DE LA PROTEíNA DE TRANSFERENCIA DE ESTERES DE COLESTEROL CETP Y SUS COMPOSICIONES FARMACÉUTICAS.

Legal Events

Date Code Title Description
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFERIMENTO DO PRESENTE PEDIDO, UMA VEZ QUE O MESMO APRESENTA REIVINDICACOES QUE ESTAO FUNDAMENTADAS NO RELATORIO DESCRITIVO E NAO DEFINEM DO MODO CLARO E PRECISO A MATERIA OBJETO DE PRETECAO ( ARTIGO 25 DA LEI 9279/96

B12B Appeal against refusal [chapter 12.2 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 02/08/2016, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 10/02/1998 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21A Patent or certificate of addition expired [chapter 21.1 patent gazette]

Free format text: PATENTE EXTINTA EM 10/02/2018

B25H Request for change of headquarter rejected

Free format text: INDEFERIDO O PEDIDO DE ALTERACAO DE SEDE CONTIDO NA PETICAO 870210027207 DE23/03/2021 DEVIDO AO DESPACHO PUBLICADO NA RPI 2630 DE 01/06/2021.