WO2003048116A3 - Esters and amides as ppar-alpha agonists ____________ - Google Patents

Esters and amides as ppar-alpha agonists ____________ Download PDF

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Publication number
WO2003048116A3
WO2003048116A3 PCT/IB2002/005064 IB0205064W WO03048116A3 WO 2003048116 A3 WO2003048116 A3 WO 2003048116A3 IB 0205064 W IB0205064 W IB 0205064W WO 03048116 A3 WO03048116 A3 WO 03048116A3
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WO
WIPO (PCT)
Prior art keywords
pharmaceutically acceptable
compounds
preparation
novel
alpha agonists
Prior art date
Application number
PCT/IB2002/005064
Other languages
French (fr)
Other versions
WO2003048116A2 (en
Inventor
Debnath Bhuniya
Saibal Kumar Das
Gurram Ranga Madhavan
Javed Iqbal
Ranjan Chakrabarti
Reeba Kannimel Vikramadithyan
Original Assignee
Reddys Lab Ltd Dr
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 to UA20040705344A priority Critical patent/UA82835C2/en
Priority to MXPA04005257A priority patent/MXPA04005257A/en
Priority to AU2002351069A priority patent/AU2002351069A1/en
Priority to EA200400762A priority patent/EA008947B1/en
Priority to EP02785781A priority patent/EP1453795A2/en
Priority to HU0402550A priority patent/HUP0402550A3/en
Priority to KR10-2004-7008538A priority patent/KR20040066866A/en
Priority to JP2003549308A priority patent/JP2005511686A/en
Priority to BR0214675-4A priority patent/BR0214675A/en
Priority to CA002469227A priority patent/CA2469227A1/en
Priority to IL16218502A priority patent/IL162185A0/en
Application filed by Reddys Lab Ltd Dr filed Critical Reddys Lab Ltd Dr
Priority to NZ533311A priority patent/NZ533311A/en
Priority to YUP-481/04A priority patent/RS48104A/en
Publication of WO2003048116A2 publication Critical patent/WO2003048116A2/en
Priority to HR20040485A priority patent/HRP20040485A2/en
Publication of WO2003048116A3 publication Critical patent/WO2003048116A3/en
Priority to NO20042805A priority patent/NO20042805L/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/06Antihyperlipidemics
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/06Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to carbon atoms of six-membered aromatic rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C211/43Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C211/44Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
    • C07C211/45Monoamines
    • C07C211/46Aniline
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
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    • C07C309/72Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/50Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52Y being a hetero atom
    • C07C311/53X and Y not being nitrogen atoms, e.g. N-sulfonylcarbamic acid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
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  • Cardiology (AREA)
  • Obesity (AREA)
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Abstract

The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to compounds of the general formula (I) which are predominantly PPAR alpha agonists, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them The present invention also relates to processes for the preparation of novel compounds of formula (I), novel intermediates, processes for their preparation, use of the novel intermediates in the preparation of the above said compounds and their use as antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds.
PCT/IB2002/005064 2001-12-03 2002-12-02 Esters and amides as ppar-alpha agonists ____________ WO2003048116A2 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
UA20040705344A UA82835C2 (en) 2001-12-03 2002-02-12 ?-aryl-?-oxysubstituted propionuc acid derivatives and pharmaceutical composition based thereon
IL16218502A IL162185A0 (en) 2001-12-03 2002-12-02 Phenylpropionate derivatives, methods for the preparation thereof and pharmaceutical compositions containing the same
CA002469227A CA2469227A1 (en) 2001-12-03 2002-12-02 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
EP02785781A EP1453795A2 (en) 2001-12-03 2002-12-02 Esters and amides as ppar-alpha agonists
AU2002351069A AU2002351069A1 (en) 2001-12-03 2002-12-02 Esters and amides as PPAR-alpha agonists
KR10-2004-7008538A KR20040066866A (en) 2001-12-03 2002-12-02 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
JP2003549308A JP2005511686A (en) 2001-12-03 2002-12-02 Novel compounds and their use in medicine, processes for their preparation and pharmaceutical compositions containing them
MXPA04005257A MXPA04005257A (en) 2001-12-03 2002-12-02 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them.
EA200400762A EA008947B1 (en) 2001-12-03 2002-12-02 PRARα AGONISTS AND USE THEREOF
HU0402550A HUP0402550A3 (en) 2001-12-03 2002-12-02 Esters and amides as ppar-alpha agonists
BR0214675-4A BR0214675A (en) 2001-12-03 2002-12-02 Novel compounds and their use in medicine, processes for their preparation and pharmaceutical compositions containing them
NZ533311A NZ533311A (en) 2001-12-03 2002-12-02 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
YUP-481/04A RS48104A (en) 2001-12-03 2002-12-02 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing theim
HR20040485A HRP20040485A2 (en) 2001-12-03 2004-05-31 New compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
NO20042805A NO20042805L (en) 2001-12-03 2004-07-02 New compounds and their use in medicine, methods of their preparation and pharmaceutical compositions containing them

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN971MA2001 2001-12-03
IN971/MAS/2001 2001-12-03

Publications (2)

Publication Number Publication Date
WO2003048116A2 WO2003048116A2 (en) 2003-06-12
WO2003048116A3 true WO2003048116A3 (en) 2004-06-10

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ID=29596806

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PCT/IB2002/005064 WO2003048116A2 (en) 2001-12-03 2002-12-02 Esters and amides as ppar-alpha agonists ____________

Country Status (21)

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US (2) US7314889B2 (en)
EP (1) EP1453795A2 (en)
JP (1) JP2005511686A (en)
KR (1) KR20040066866A (en)
CN (1) CN1697828A (en)
AU (1) AU2002351069A1 (en)
BR (1) BR0214675A (en)
CA (1) CA2469227A1 (en)
CO (1) CO5580760A2 (en)
EA (1) EA008947B1 (en)
HR (1) HRP20040485A2 (en)
HU (1) HUP0402550A3 (en)
IL (1) IL162185A0 (en)
MX (1) MXPA04005257A (en)
NO (1) NO20042805L (en)
NZ (1) NZ533311A (en)
PL (1) PL370554A1 (en)
RS (1) RS48104A (en)
UA (1) UA82835C2 (en)
WO (1) WO2003048116A2 (en)
ZA (1) ZA200404261B (en)

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