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WO2003002531A3 - Fluoropyrrolidines as dipeptidyl peptidase inhibitors - Google Patents

Fluoropyrrolidines as dipeptidyl peptidase inhibitors Download PDF

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Publication number
WO2003002531A3
WO2003002531A3 PCT/US2002/020471 US0220471W WO03002531A3 WO 2003002531 A3 WO2003002531 A3 WO 2003002531A3 US 0220471 W US0220471 W US 0220471W WO 03002531 A3 WO03002531 A3 WO 03002531A3
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WO
WIPO (PCT)
Prior art keywords
dipeptidyl peptidase
fluoropyrrolidines
peptidase inhibitors
dipeptidyl
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2002/020471
Other languages
French (fr)
Other versions
WO2003002531A2 (en
Inventor
Curt Dale Haffner
Darryl Lynn Mcdougald
Amarjit Sab Randhawa
Steven Michael Reister
James Martin Lenhard
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 NZ529973A priority Critical patent/NZ529973A/en
Priority to IL15892302A priority patent/IL158923A0/en
Priority to JP2003508714A priority patent/JP3909056B2/en
Priority to MXPA03011907A priority patent/MXPA03011907A/en
Priority to KR10-2003-7016958A priority patent/KR20040015298A/en
Priority to AU2002322344A priority patent/AU2002322344C1/en
Priority to US10/481,293 priority patent/US7132443B2/en
Priority to EP02756329A priority patent/EP1406873B1/en
Priority to CA002450722A priority patent/CA2450722A1/en
Application filed by SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Priority to HU0400321A priority patent/HUP0400321A2/en
Priority to BR0210644-2A priority patent/BR0210644A/en
Priority to DE60222667T priority patent/DE60222667T2/en
Publication of WO2003002531A2 publication Critical patent/WO2003002531A2/en
Publication of WO2003002531A3 publication Critical patent/WO2003002531A3/en
Priority to NO20035603A priority patent/NO20035603D0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system

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Abstract

The present invention relates to novel compounds of formula (I): , their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.
PCT/US2002/020471 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors Ceased WO2003002531A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
CA002450722A CA2450722A1 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
JP2003508714A JP3909056B2 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
MXPA03011907A MXPA03011907A (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors.
KR10-2003-7016958A KR20040015298A (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
AU2002322344A AU2002322344C1 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US10/481,293 US7132443B2 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
EP02756329A EP1406873B1 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
NZ529973A NZ529973A (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
HU0400321A HUP0400321A2 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors and pharmaceutical compositions containing them
IL15892302A IL158923A0 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
BR0210644-2A BR0210644A (en) 2001-06-27 2002-06-26 Compound, pharmaceutical formulation, method for inhibiting a proline / alanine cleaving protease, method for treatment or prophylaxis of disorders, and use of the compound
DE60222667T DE60222667T2 (en) 2001-06-27 2002-06-26 FLUORPYRROLIDINES AS DIPEPTIDYLPEPTIDASE INHIBITORS
NO20035603A NO20035603D0 (en) 2001-06-27 2003-12-16 Fluoropyrrolidines as dipeptidyl peptidase inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US30133301P 2001-06-27 2001-06-27
US60/301,333 2001-06-27
US37601502P 2002-04-26 2002-04-26
US60/376,015 2002-04-26

Publications (2)

Publication Number Publication Date
WO2003002531A2 WO2003002531A2 (en) 2003-01-09
WO2003002531A3 true WO2003002531A3 (en) 2003-04-03

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PCT/US2002/020471 Ceased WO2003002531A2 (en) 2001-06-27 2002-06-26 Fluoropyrrolidines as dipeptidyl peptidase inhibitors

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US (1) US7132443B2 (en)
EP (2) EP1406873B1 (en)
JP (3) JP3909056B2 (en)
KR (1) KR20040015298A (en)
CN (3) CN1990468A (en)
AT (2) ATE374181T1 (en)
AU (1) AU2002322344C1 (en)
BR (1) BR0210644A (en)
CA (1) CA2450722A1 (en)
CO (1) CO5600998A2 (en)
CZ (1) CZ20033521A3 (en)
DE (2) DE60222667T2 (en)
ES (2) ES2339813T3 (en)
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US20040171848A1 (en) 2004-09-02
CN1990468A (en) 2007-07-04
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CZ20033521A3 (en) 2004-05-12
EP1862457A3 (en) 2008-02-20
DE60222667T2 (en) 2008-07-17
CN1723196A (en) 2006-01-18
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CA2450722A1 (en) 2003-01-09
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JP2004535445A (en) 2004-11-25
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BR0210644A (en) 2004-07-20
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