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
  • C07D213/78—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
  • C07D213/82—Amides; Imides in position 3
• • 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
  • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P13/00—Drugs for disorders of the urinary system
  • A61P13/12—Drugs for disorders of the urinary system of the kidneys
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
• • 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
  • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
  • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P37/00—Drugs for immunological or allergic disorders
• • 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
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
  • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
  • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• • 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
  • C07D417/02—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 two hetero rings
  • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Definitions

• the present invention relates to a class of compounds of pyridinium series
• the invention relates to compounds of this series, methods for their preparation,
• kidney disease aging-related complications including kidney disease, nerve damage,
• the invention also provides a means for treating atherosclerosis, retinopathy and dermatological conditions.
• the invention also provides a means for treating atherosclerosis, retinopathy and dermatological conditions.
• Maillard reaction occurs in two stages, early and advanced. Initially, proteins react with glucose to form stable Amadori products,
• diabetes such as nephropathy
• reducing sugars such as ribose or glucose with bovine serum albumin.
• the AGE derived protein cross-links have been shown to be cleaved by compounds like N- phenacyl thiazoUum bromide (PTB), which
• aminoguanidine which acts slowly by its very
• the main objective of the present invention is to provide a class of
• kidney disease including kidney disease, nerve damage, atherosclerosis, retinopathy and
• the invention also extends the method to reverse the
• Another object of the present invention is to provide compounds of the
• Yet another object of the present invention is to provide a method of
• Still another object of the invention is to provide pharmaceutical
• compositions with a new class of compounds of the pyridinium series according to
• compositions employed in preparing such compositions.
• Still another object of the invention is to provide a method of treatment of a
• the present invention provides for a new class of AGE breakers, of general
• R 1 is -Y-R 3
• Y is selected from oxygen or NH.
• R 3 is selected from hydrogen, alkyl, aryl
• R 2 is selected from group consisting of alkyl, -Oalkyl, aryl, -Oaryl, -NHalkyl and
• X is selected from group consisting of a halide ion, acetate ion, perchlorate ion,
• R 1 is other than -OCH 3 .
• alkyl refers to an optionally substituted, saturated
• the saturated alkyl hydrocarbon group may be linear or
• aryl refers to an optionally substituted aromatic group
• Aryl includes carbocyclic aryl and heterocyclic
• the present invention provides a plurality of the present invention.
• kidney disease amputations including kidney disease, nerve damage, atherosclerosis,
• preformed AGE the higher levels of preformed AGE.
• the increased levels of preformed AGE can be
• the invention also provides a process for the preparation of compounds of
• the said process for the preparation of compound 1, comprises, adding a
• Bovine serum albumin fraction V (BSA)
• PBS Phosphate buffered saline
• Microplate ELISA Reader - Spectramax Plus (Molecular Devices, USA) Microplate washer, (Bio -Tec Instruments, USA)
• test samples were coated on microtitre plate at a concentration of 5 ng. to
• the plate was washed with PBST.
• the breaker activity of the compounds were determined by the following
• compound 12 has significant AGE - breaking activity i.e. a
• Nicotinamide (1.22g, 0.01 mol) was dissolved in refluxing toluene (40 ml)
• the precipitated sohd was filtered and dissolved in methanol, decolourized with
• reagents by refluxing in alcoholic solvents like methanol, ethanol, propanol, etc.
• compositions may be prepared with a pharmaceutically
• Oral formulations may be administered as solid dosage forms for example
• pellets, powders, sachets or discreet units such as tablets or capsules and like.
• compositions include monophasic and
• biphasic liquid dosage forms either in ready to use form or forms suitable for
• preparations in addition may contain diluents, dispersing agents, buffers,
• thickening agent or suspending agent or emulsifying agent may be present in
• the compounds may be administered as such in their pure
• compositions can have a slow,
• inert excipients as are used in the art.
• Diluents such as starch, lactose, dicalcium phosphate, talc, magnesium stearate, polymeric substances like methyl cellulose,
• fatty acids and derivatives sodium starch glycollate, etc. may also be used.
• a typical tablet has the following composition:
• a sterile vehicle which may be an aqueous
• non aqueous vehicle or non aqueous vehicle or a combination thereof.
• the examples of vehicles are
• additives common in injectable preparations like stabilizers
• solubilizers pH modifiers, buffers, antioxidants, cosolvents, complexing agents,
• tonicity modifiers etc.
• suitable additives are for example tartrate, citrate or similar buffers,
• the compound may be administered
• Preparation suitable for parenteral administration has the following

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Veterinary Medicine (AREA)
• General Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Diabetes (AREA)
• Urology & Nephrology (AREA)
• Cardiology (AREA)
• Heart & Thoracic Surgery (AREA)
• Hematology (AREA)
• Obesity (AREA)
• Immunology (AREA)
• Ophthalmology & Optometry (AREA)
• Dermatology (AREA)
• Endocrinology (AREA)
• Vascular Medicine (AREA)
• Neurology (AREA)
• Biomedical Technology (AREA)
• Neurosurgery (AREA)
• Emergency Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Pyridine Compounds (AREA)
• Plural Heterocyclic Compounds (AREA)
• Medicinal Preparation (AREA)
• Cosmetics (AREA)

Applications Claiming Priority (3)

Publications (1)

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Family Applications (1)

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Family Cites Families (9)

• 1999
  • 1999-10-15 WO PCT/IB1999/001687 patent/WO2001025209A1/en not_active Application Discontinuation
  • 1999-10-15 CZ CZ20011808A patent/CZ20011808A3/cs unknown
  • 1999-10-15 EP EP99974071A patent/EP1220843A1/en not_active Withdrawn
  • 1999-10-15 CN CN99814055A patent/CN1329597A/zh active Pending
  • 1999-10-15 BR BR9915962-7A patent/BR9915962A/pt not_active IP Right Cessation
  • 1999-10-15 MX MXPA02003496A patent/MXPA02003496A/es unknown
  • 1999-10-15 AU AU59944/99A patent/AU5994499A/en not_active Abandoned
  • 1999-10-15 CA CA002351075A patent/CA2351075A1/en not_active Abandoned
  • 1999-10-15 PL PL99348049A patent/PL348049A1/xx not_active Application Discontinuation
  • 1999-10-15 HU HU0301687A patent/HUP0301687A2/hu unknown
  • 1999-10-15 JP JP2001528155A patent/JP2003511370A/ja active Pending
• 2002
  • 2002-08-12 HK HK02105890.8A patent/HK1044336A1/zh unknown

Non-Patent Citations (1)

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