WO2002102313A2 - Pyrimidine inhibitors of phosphodiesterase (pde) 7 - Google Patents

Pyrimidine inhibitors of phosphodiesterase (pde) 7 Download PDF

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Publication number
WO2002102313A2
WO2002102313A2 PCT/US2002/019097 US0219097W WO02102313A2 WO 2002102313 A2 WO2002102313 A2 WO 2002102313A2 US 0219097 W US0219097 W US 0219097W WO 02102313 A2 WO02102313 A2 WO 02102313A2
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WO
WIPO (PCT)
Prior art keywords
alkyl
optionally substituted
heteroaryl
groups
heterocyclo
Prior art date
Application number
PCT/US2002/019097
Other languages
English (en)
French (fr)
Other versions
WO2002102313A3 (en
Inventor
Junqing Guo
Joseph Barbosa
William John Pitts
Marianne Carlsen
Claude Quesnelle
Marco Dodier
Original Assignee
Bristol-Myers Squibb Company
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 Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Priority to JP2003504902A priority Critical patent/JP2005500294A/ja
Priority to CA002450934A priority patent/CA2450934A1/en
Priority to EP02744381A priority patent/EP1397142A4/en
Priority to HU0402352A priority patent/HUP0402352A2/hu
Publication of WO2002102313A2 publication Critical patent/WO2002102313A2/en
Publication of WO2002102313A3 publication Critical patent/WO2002102313A3/en

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    • 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
    • C07D417/14—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 three or more hetero 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
PCT/US2002/019097 2001-06-19 2002-06-17 Pyrimidine inhibitors of phosphodiesterase (pde) 7 WO2002102313A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2003504902A JP2005500294A (ja) 2001-06-19 2002-06-17 ホスホジエステラーゼ７に対するピリミジン阻害剤
CA002450934A CA2450934A1 (en) 2001-06-19 2002-06-17 Pyrimidine inhibitors of phosphodiesterase (pde) 7
EP02744381A EP1397142A4 (en) 2001-06-19 2002-06-17 PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7
HU0402352A HUP0402352A2 (hu) 2001-06-19 2002-06-17 Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US29928701P 2001-06-19 2001-06-19
US60/299,287 2001-06-19
US35514102P 2002-02-08 2002-02-08
US60/355,141 2002-02-08
US36875202P 2002-03-29 2002-03-29
US60/368,752 2002-03-29

Publications (2)

Publication Number Publication Date
WO2002102313A2 true WO2002102313A2 (en) 2002-12-27
WO2002102313A3 WO2002102313A3 (en) 2003-04-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/019097 WO2002102313A2 (en) 2001-06-19 2002-06-17 Pyrimidine inhibitors of phosphodiesterase (pde) 7

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US (1) US7087614B2 (US20030162802A1-20030828-C00106.png)
EP (1) EP1397142A4 (US20030162802A1-20030828-C00106.png)
JP (1) JP2005500294A (US20030162802A1-20030828-C00106.png)
CA (1) CA2450934A1 (US20030162802A1-20030828-C00106.png)
HU (1) HUP0402352A2 (US20030162802A1-20030828-C00106.png)
WO (1) WO2002102313A2 (US20030162802A1-20030828-C00106.png)

Cited By (81)

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WO2004048365A1 (en) * 2002-11-21 2004-06-10 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer
WO2004087679A1 (en) * 2003-04-01 2004-10-14 Aponetics Ag 2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases
DE102004049622A1 (de) * 2004-10-06 2006-04-20 Schering Ag Subtituierte 2-Anilinopyrimidine als Zellzyklus-kinase oder Rezeptortyrosin-kinase Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
JP2008505876A (ja) * 2004-07-09 2008-02-28 アストラゼネカ アクチボラグ ホスファチジルイノシトール（ｐｉ）３−キナーゼ阻害剤としての２，４，６−三置換ピリミジンおよび癌の治療におけるその使用
EP1951261A2 (en) * 2005-10-31 2008-08-06 Rigel Pharmaceuticals, Inc. Compositions and methods for treating inflammatory disorders
US7491732B2 (en) 2005-06-08 2009-02-17 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7655797B2 (en) 2002-02-01 2010-02-02 Rigel Pharmaceuticals, Inc. Intermediates for making 2,4-pyrimidinediamine compounds
US7659280B2 (en) 2006-02-17 2010-02-09 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
US7696204B2 (en) 2005-10-11 2010-04-13 Ludwig Institute For Cancer Research Pharmaceutical compounds
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
US7812029B1 (en) 2002-07-29 2010-10-12 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7851480B2 (en) 2004-11-24 2010-12-14 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
US7863286B2 (en) 2004-11-15 2011-01-04 Rigel Pharmaceuticals, Inc. Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
WO2011015641A1 (en) * 2009-08-05 2011-02-10 Katholieke Universiteit Leuven Novel viral replication inhibitors
US7928109B2 (en) 2007-04-18 2011-04-19 Pfizer Inc Sulfonyl amide derivatives for the treatment of abnormal cell growth
US8173647B2 (en) 2007-02-06 2012-05-08 Gordana Atallah PI 3-kinase inhibitors and methods of their use
WO2012064667A2 (en) 2010-11-08 2012-05-18 Omeros Corporation Treatment of addiction and impulse-control disorders using pde7 inhibitors
US8217035B2 (en) 2006-01-20 2012-07-10 Novartis Ag Pyrimidine derivatives used as PI-3-kinase inhibitors
US8354420B2 (en) 2010-06-04 2013-01-15 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 inhibitors
US8410119B2 (en) 2003-07-14 2013-04-02 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2013146963A1 (ja) 2012-03-28 2013-10-03 武田薬品工業株式会社 複素環化合物
US8551984B2 (en) 2009-12-17 2013-10-08 Merck Sharp & Dohme Corp. Aminopyrimidines as SYK inhibitors
US8637528B2 (en) 2007-03-27 2014-01-28 Omeros Corporation Use of PDE7 inhibitors for the treatment of movement disorders
US8716281B2 (en) 2010-05-11 2014-05-06 Amgen Inc. Pyrimidine compounds that inhibit anaplastic lymphoma kinase
US8735417B2 (en) 2009-12-17 2014-05-27 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
US8785638B2 (en) 2009-05-15 2014-07-22 Katholieke Universiteit Leuven Thieno [2, 3-B] pyridine derivatives as viral replication inhibitors
US8815882B2 (en) 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators
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