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1. 发明申请

US20080058359A1 Piperidinyl compounds that selectively bind integrins 有权
标题翻译：选择性结合整联蛋白的哌啶基化合物
公开(公告)号：US20080058359A1
公开(公告)日：2008-03-06
申请号：US11897484
申请日：2007-08-30
申请人： Bart De Corte , William Kinney , Bruce Maryanoff , Shyamali Ghosh , Li Liu
发明人： Bart De Corte , William Kinney , Bruce Maryanoff , Shyamali Ghosh , Li Liu
IPC分类号： A61K31/4545 , A61K31/4375 , A61K31/506 , A61P17/00 , A61P19/00 , A61P27/00 , A61P35/00 , C07D401/12 , C07D401/14 , C07D471/04
CPC分类号： C07D471/04 , A61K31/4523 , A61K45/06 , A61K51/0455 , A61K51/0459 , C07D401/12 , C07D401/14 , C07D405/14 , Y02P20/582 , A61K2300/00
摘要： The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.
摘要翻译：本发明涉及选择性结合整联蛋白受体的哌啶基化合物和用于治疗整联蛋白介导的病症的方法。

2. 发明授权

US08110683B2 Piperidinyl compounds that selectively bind integrins 有权
标题翻译：选择性结合整联蛋白的哌啶基化合物
公开(公告)号：US08110683B2
公开(公告)日：2012-02-07
申请号：US12975900
申请日：2010-12-22
申请人： Bart De Corte , William A. Kinney , Bruce E. Maryanoff , Shyamali Ghosh , Li Liu
发明人： Bart De Corte , William A. Kinney , Bruce E. Maryanoff , Shyamali Ghosh , Li Liu
IPC分类号： C07D239/06
CPC分类号： C07D471/04 , A61K31/4523 , A61K45/06 , A61K51/0455 , A61K51/0459 , C07D401/12 , C07D401/14 , C07D405/14 , Y02P20/582 , A61K2300/00
摘要： The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.
摘要翻译：本发明涉及选择性结合整联蛋白受体的哌啶基化合物和用于治疗整联蛋白介导的病症的方法。

3. 发明授权

US07879881B2 Piperidinyl compounds that selectively bind integrins 有权
标题翻译：选择性结合整联蛋白的哌啶基化合物
公开(公告)号：US07879881B2
公开(公告)日：2011-02-01
申请号：US11897484
申请日：2007-08-30
申请人： Bart De Corte , William A. Kinney , Bruce E. Maryanoff , Shyamali Ghosh , Li Liu
发明人： Bart De Corte , William A. Kinney , Bruce E. Maryanoff , Shyamali Ghosh , Li Liu
IPC分类号： A61K31/452 , C07D211/32
CPC分类号： C07D471/04 , A61K31/4523 , A61K45/06 , A61K51/0455 , A61K51/0459 , C07D401/12 , C07D401/14 , C07D405/14 , Y02P20/582 , A61K2300/00
摘要： The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.
摘要翻译：本发明涉及选择性结合整联蛋白受体的哌啶基化合物和用于治疗整联蛋白介导的病症的方法。

4. 发明申请

US20110092528A1 PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS 有权
标题翻译： PIPERIDINYL化合物选择性结合
公开(公告)号：US20110092528A1
公开(公告)日：2011-04-21
申请号：US12975900
申请日：2010-12-22
申请人： Bart De Corte , Willam A. Kinney , Bruce E. Maryanolf , Shyamali Ghosh , Li Liu
发明人： Bart De Corte , Willam A. Kinney , Bruce E. Maryanolf , Shyamali Ghosh , Li Liu
IPC分类号： A61K31/506 , C07D401/12 , C07D401/14 , C07D471/04 , A61K31/4375
CPC分类号： C07D471/04 , A61K31/4523 , A61K45/06 , A61K51/0455 , A61K51/0459 , C07D401/12 , C07D401/14 , C07D405/14 , Y02P20/582 , A61K2300/00
摘要： The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.
摘要翻译：本发明涉及选择性结合整联蛋白受体的哌啶基化合物和用于治疗整联蛋白介导的病症的方法。

5. 发明申请

US20070015207A1 Triazolopyrimidine derivatives 有权
标题翻译：三唑并嘧啶衍生物
公开(公告)号：US20070015207A1
公开(公告)日：2007-01-18
申请号：US11329642
申请日：2006-01-11
申请人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
发明人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C12N5/06 , C07D487/02 , C07K16/40 , C12N9/12
CPC分类号： C07K14/4738 , C07D487/04 , C12N9/1205 , C12Q1/485 , G01N2500/02
摘要： The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
摘要翻译：本发明涉及已发现对丝氨酸 - 酪氨酸和酪氨酸激酶具有抑制活性的式（I）三唑并嘧啶衍生物的发现。

6. 发明申请

US20050234117A1 Triazoles as farnesyl transferase inhibitors 有权
公开(公告)号：US20050234117A1
公开(公告)日：2005-10-20
申请号：US11143814
申请日：2005-06-02
申请人： Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
发明人： Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
IPC分类号： A61K31/4196 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61P1/00 , A61P1/18 , A61P11/00 , A61P13/10 , A61P13/12 , A61P17/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

7. 发明申请

US20080103150A1 Triazoles as Farnesyl Transferase Inhibitors 有权
公开(公告)号：US20080103150A1
公开(公告)日：2008-05-01
申请号：US11926858
申请日：2007-10-29
申请人： Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
发明人： Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
IPC分类号： A61K31/4196 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61K31/506 , A61K31/53 , A61P35/00 , C07D249/08 , C07D401/12 , C07D403/12
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

8. 发明申请

US20110263625A1 HIV REPLICATION INHIBITING PYRIMIDINES 有权
公开(公告)号：US20110263625A1
公开(公告)日：2011-10-27
申请号：US13177188
申请日：2011-07-06
申请人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
发明人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
IPC分类号： A61K31/505 , A61P31/18 , C07D239/50 , C07D239/48 , C07D239/47
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

9. 发明授权

US08003789B2 HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶
公开(公告)号：US08003789B2
公开(公告)日：2011-08-23
申请号：US11930835
申请日：2007-10-31
申请人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
发明人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61P31/18
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.
摘要翻译：本发明涉及式I化合物的N-氧化物，药学上可接受的加成盐，季胺，其立体化学异构体形式的用途，其中-a1 = a2-a3 = a4形成苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基，乙烯基; n为0〜5; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基，取代的C 1-6烷基，取代的C 1-6烷氧基C 1-6烷基羰基; R2是羟基，卤素，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 3-7环烷基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或二（C 1-6烷基）氨基，多卤代甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，5元杂环; L是任选取代的C 1-10烷基，C 2-10烯基，C 2-10炔基或C 3-7环烷基; 或-X-R 3; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基，任选取代的氨基; Y表示羟基，卤素，C 3-7环烷基，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单 - 或二（C 1-6烷基）氨基，多卤甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，芳基; 用于治疗患有艾滋病毒感染的受试者。

10. 发明授权

US07037917B2 HIV replication inhibiting pyrimidines 有权
公开(公告)号：US07037917B2
公开(公告)日：2006-05-02
申请号：US10634682
申请日：2003-08-05
申请人： Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： C07D239/48 , A61K31/506 , A61P31/18
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

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