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1. 发明申请

US20060183747A1 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
公开(公告)号：US20060183747A1
公开(公告)日：2006-08-17
申请号：US10565065
申请日：2004-07-12
申请人： Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
发明人： Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; or optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X1 represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents optionally substituted C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one hetetoatom selected from O, S or N; benzoxazolyl or a radical of formula X2 represents a direct bond; —NR1—; —NR1—(CH2)n3—; —O—; —O—(CH2)n3—; —C(═O)—; —C(═O)—(CH2)n3—; —C(═O)—NR5—(CH2)n3—; —C(═S)—; —S—; —S(═O)n1—; —(CH2)n3—; —(CH2)n4—X1a—X1b—; —X1a—X1b—(CH2)n4—; —S(═O)n1—NR5—(CH2)n3—NR5— or —S(═O)n1—NR5—(CH2)n3—; R3 represents an optionally substituted 5- or 6-membered monocyclic heterocycle containing at least one heteroatom selected from O, S or N, or a 9- or 10-membered bicyclic heterocycle containing at least one heteroatom selected from O, S or N; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; optionally substituted C2-4alkenyl or C2-4alkynyl; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR9R10; C(═O)NR9R10; —NR5—C(═O)—NR9R10; —NR5—C(═O)—R11; —S(═O)n1—R11; —NR5—S(═O)n1—R11; —S—CN; —NR5—CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

2. 发明申请

US20070078132A1 Pyrido-and pyrimidopyrimidine derivatives as anti-profilerative agents 有权
公开(公告)号：US20070078132A1
公开(公告)日：2007-04-05
申请号：US10596512
申请日：2004-12-15
申请人： Eddy Freyne , Marc Willems , Pierre Storck , Virginie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Buijnsters , Werner Embrechts , Timothy Perera
发明人： Eddy Freyne , Marc Willems , Pierre Storck , Virginie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Buijnsters , Werner Embrechts , Timothy Perera
IPC分类号： A61K31/5377 , A61K31/535 , A61K31/525 , C07D491/22
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

3. 发明申请

US20050239784A1 3-Phenyl analogs of toxoflavine as kinase inhibitors 审中-公开
公开(公告)号：US20050239784A1
公开(公告)日：2005-10-27
申请号：US10520768
申请日：2003-07-08
申请人： Jean LaCrampe , Richard Connors , Chih Ho , Alan Ricardson , Eddy Freyne , Peter Jacobus Buijnsters , Annette Bakker
发明人： Jean LaCrampe , Richard Connors , Chih Ho , Alan Ricardson , Eddy Freyne , Peter Jacobus Buijnsters , Annette Bakker
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07D487/02
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C1-4alkyl; R represents C1-4alkyl; R3 represents C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het1 wherein said C3-8cycloalkyl or Het1 each independently may optionally be substituted with C1-4alkyloxycarbonyl; R4 represents halo or C1-4alkyloxy; R5 represents C1-4alkyloxycarbonyl, —O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het3 or NR6R7, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het4 or NR8R9; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het5; R8 and R9 are each independently selected from hydrogen, C1-4alkyl, -Het7 or mono- or di(C1-4alkyl)aminosulphonyl; Het3 represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(C1-4alkyl)aminosulfonyl; Het7 represents piperidinyl.

4. 发明申请

US20050090495A1 Novel IL-5 inhibiting 6-azauracil derivatives for marking and identifying receptors and imaging organs 审中-公开
公开(公告)号：US20050090495A1
公开(公告)日：2005-04-28
申请号：US10671205
申请日：2003-09-25
申请人： Jean Lacrampe , Eddy Freyne , Marc Venet , Gustaaf Boeckx
发明人： Jean Lacrampe , Eddy Freyne , Marc Venet , Gustaaf Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , A61K31/53
CPC分类号： C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4allyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R3, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

5. 发明申请

US20080070914A1 5-Membered Annelated Heterocyclic Pyrimidines As Kinase Inhibitors 有权
标题翻译：作为激酶抑制剂的5-Membined Annelated Heterocyclic Pyrimidines
公开(公告)号：US20080070914A1
公开(公告)日：2008-03-20
申请号：US11813656
申请日：2006-01-09
申请人： Eddy Freyne , Jean Lacrampe , Timothy Perera , Peter Ten Holte , Yannick Ligny , Delphine Lardeau , Tom Lavrijssen
发明人： Eddy Freyne , Jean Lacrampe , Timothy Perera , Peter Ten Holte , Yannick Ligny , Delphine Lardeau , Tom Lavrijssen
IPC分类号： A61K31/497 , A61K31/535 , A61P43/00 , C07D413/00 , C07D473/00
CPC分类号： C07D473/32 , C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and Z have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4， >，R 5，R 6，Q 1，Q 2，X 1，...，SUP Y，Z定义含有细胞周期激酶抑制酶活性，其制备方法，含有它们的组合物及其作为药物的用途。

6. 发明申请

US20060040943A1 3-Furanyl analogs of toxoflavine as kinase inhibitors 失效
公开(公告)号：US20060040943A1
公开(公告)日：2006-02-23
申请号：US10520641
申请日：2003-07-08
申请人： Jean Fernand LaCrampe , Richard Connors , Chih Ho , Alan Richardson , Eddy Freyne , Peter Buijnsters , Annette Bakker
发明人： Jean Fernand LaCrampe , Richard Connors , Chih Ho , Alan Richardson , Eddy Freyne , Peter Buijnsters , Annette Bakker
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R1 represents C1-4alkyl, C1-4alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C1-4alkyloxycarbonyl; R2 represents hydrogen or C1-4alkyl; R3 represents hydrogen or C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C1-4alkyloxycarbonyl, phenylcarbonyl or —C(═NH)—NH2; R4 represents halo or C1-4alkyloxy; R5 represents Het2, C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het3 or NR6R7, or C1-4alkyloxy substituted with one or where possible more substituents being selected from Het4 or —C(═O)-Het4; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy or Het5; Het2 represents piperazinyl; Het3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl preferably methyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl, C1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C1-4alkyl substituents, preferably methyl; Het5 represents a heterocycle selected from pyridinyl, pyrrolidinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl.

7. 发明申请

US20080039477A1 Pyrazolopyrimidines as Cell Cycle Kinase Inhibitors 有权
标题翻译：吡唑并嘧啶作为细胞周期激酶抑制剂
公开(公告)号：US20080039477A1
公开(公告)日：2008-02-14
申请号：US11813654
申请日：2006-01-09
申请人： Eddy Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aime Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
发明人： Eddy Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aime Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
IPC分类号： A61K31/52 , A61P35/00 , C07D473/00
CPC分类号： C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4， >，R 5，R 6，X 1和X 2具有定义的含义，具有抑制细胞周期激酶酶活性，它们的制备，含有它们的组合物及其作为药物的用途。

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