公开(公告)号：WO2007050087A1

公开(公告)日：2007-05-03

申请号：PCT/US2005/039294

申请日：2005-10-28

Applicant: VALEANT RESEARCH & DEVELOPMENT ,  GIRARDET, Jean-luc ,  KOH, Yung-hyo ,  DE LA ROSA, Martha ,  HONG, Zhi ,  LANG, Stanley

Inventor： GIRARDET, Jean-luc ,  KOH, Yung-hyo ,  DE LA ROSA, Martha ,  HONG, Zhi ,  LANG, Stanley

IPC: A61K31/4196 ,  C07D249/08

CPC classification number: C07D249/12 ,  C07D249/14

Abstract: A series of S-triazolyl α-mercaptoacetanilides having N-(a-mercaptoacetyl) p amino benzoic acid derivatives are provided, where Q is CO 2 H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.

Abstract translation: 提供了一系列具有N-（α-巯基乙酰基）p氨基苯甲酸衍生物的S-三唑基α-巯基乙酰替苯胺，其中Q为CO 2 H，或其盐或酯，或C（ O）N-连接的氨基酸。 这些化合物抑制HIV的逆转录酶的几种变体，并且可用于治疗HIV感染。

公开(公告)号：WO2006122003A3

公开(公告)日：2007-01-04

申请号：PCT/US2006017677

申请日：2006-05-05

Applicant: VALEANT RES & DEV ,  GIRARDET JEAN LUC ,  KOH YUNG-HYO ,  SHAW STEPHANIE ,  KIN HONG WOO

Inventor： GIRARDET JEAN LUC ,  KOH YUNG-HYO ,  SHAW STEPHANIE ,  KIN HONG WOO

IPC: C07D487/04 ,  C07D473/30 ,  C07D473/34 ,  C07D473/38

CPC classification number: C07D487/04 ,  C07D473/30

Abstract: This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6- arylthio- purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

Abstract translation: 本申请涉及某些2-苯基氨基-6-芳基氨基，6-芳氧基和6-芳硫基嘌呤，氮杂嘌呤和脱氮嘌呤。 这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。

公开(公告)号：WO2004030611A3

公开(公告)日：2004-06-17

申请号：PCT/US0327433

申请日：2003-08-22

Applicant: RIBAPHARM INC ,  GIRARDET JEAN-LUC ,  ZHANG ZHIJUN ,  HAMATAKE ROBERT ,  HERNANDEZ MARTHA DE LA ROSA ,  GUNIC ESMIR ,  HONG ZHI ,  KIM HONGWOO ,  KOH YUNG-HYO ,  NILAR SHAHUL ,  SHAW STEPHANIE ,  YAO NANHUA

Inventor： GIRARDET JEAN-LUC ,  ZHANG ZHIJUN ,  HAMATAKE ROBERT ,  HERNANDEZ MARTHA DE LA ROSA ,  GUNIC ESMIR ,  HONG ZHI ,  KIM HONGWOO ,  KOH YUNG-HYO ,  NILAR SHAHUL ,  SHAW STEPHANIE ,  YAO NANHUA

IPC: A61K31/13 ,  A61K31/4196 ,  A61K31/4709 ,  C07D233/84 ,  C07D249/08 ,  C07D249/10 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  A01N33/02

CPC classification number: C07D249/08 ,  A61K31/4196 ,  A61K31/4709 ,  C07D233/84 ,  C07D249/10 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

Abstract: Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds.

Abstract translation: 各种羰基酰胺在体外和体内被用作逆转录酶的非核苷抑制剂，特别是HIV逆转录酶的非核苷抑制剂。 因此，预期的化合物可用于治疗HIV感染患者。 进一步考虑的方面包括包含治疗有效量的预期化合物的药物组合物。

公开(公告)号：WO03051881B1

公开(公告)日：2003-08-28

申请号：PCT/US0240414

申请日：2002-12-17

Applicant: RIBAPHARM INC ,  AN HAOYUN ,  GUNIC ESMIR ,  KOH YUNG-HYO ,  CHEN HUANMING ,  BARAWKAR DINESH ,  ZHANG WEIJIAN ,  GIRARDET JEAN-LUC ,  RONG FRANK ,  HONG ZHI

Inventor： AN HAOYUN ,  GUNIC ESMIR ,  KOH YUNG-HYO ,  CHEN HUANMING ,  BARAWKAR DINESH ,  ZHANG WEIJIAN ,  GIRARDET JEAN-LUC ,  RONG FRANK ,  HONG ZHI

IPC: C07B61/00 ,  C07D473/00 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00

CPC classification number: C07D473/00 ,  C07B2200/11 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C40B40/00

Abstract: Nucleoside analog libraries are prepared in a combinatorial library approach. In some preferred aspects, library diversity is generated using solid phase-coupled nucleosides in a series of at least two modification reactions, and contemplated libraries and compounds include various 2-C-substituted purines, 3-deoxy/aza-6-substituted purines, substituted 2-thioadenosines, 2-amino-6,8-disubstituted purines, 2,8-disubstituted guanosines, 6-substituted purines, 2,6-disubstituted adenosines, and 6,8-disubstituted adenosines. Particularly preferred compounds include nucleoside analogs generated using contemplated libraries, which may be useful in treatment of various conditions, particularly viral infections and neoplastic diseases.

Abstract translation: 核苷类似物文库以组合文库方法制备。 在一些优选的方面，使用固相耦合的核苷在一系列至少两个修饰反应中产生文库多样性，并且考虑的文库和化合物包括各种2-C-取代的嘌呤，3-脱氧/氮杂-6-取代的嘌呤， 取代的2-硫代腺苷，2-氨基-6,8-二取代的嘌呤，2,8-二取代的鸟苷，6-取代的嘌呤，2,6-二取代的腺苷和6,8-二取代的腺苷。 特别优选的化合物包括使用考虑的文库产生的核苷类似物，其可用于治疗各种病症，特别是病毒感染和肿瘤疾病。

公开(公告)号：WO2003051881A1

公开(公告)日：2003-06-26

申请号：PCT/US2002/040414

申请日：2002-12-17

Applicant: RIBAPHARM INC. ,  AN, Haoyun ,  GUNIC, Esmir ,  KOH, Yung-hyo ,  CHEN, Huanming ,  BARAWKAR, Dinesh ,  ZHANG, Weijian ,  GIRARDET, Jean-Luc ,  RONG, Frank ,  HONG, Zhi

Inventor： AN, Haoyun ,  GUNIC, Esmir ,  KOH, Yung-hyo ,  CHEN, Huanming ,  BARAWKAR, Dinesh ,  ZHANG, Weijian ,  GIRARDET, Jean-Luc ,  RONG, Frank ,  HONG, Zhi

IPC: C07D473/00

CPC classification number: C07D473/00 ,  C07B2200/11 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C40B40/00

Abstract: Nucleoside analog libraries are prepared in a combinatorial library approach. In some preferred aspects, library diversity is generated using solid phase-coupled nucleosides in a series of at least two modification reactions, and contemplated libraries and compounds include various 2-C-substituted purines, 3-deoxy/aza-6-substituted purines, substituted 2-thioadenosines, 2-amino-6,8-disubstituted purines, 2,8-disubstituted guanosines, 6-substituted purines, 2,6-disubstituted adenosines, and 6,8-disubstituted adenosines. Particularly preferred compounds include nucleoside analogs generated using contemplated libraries, which may be useful in treatment of various conditions, particularly viral infections and neoplastic diseases.

Abstract translation: 在组合文库方法中制备核苷类似物文库。 在一些优选的方面，使用一系列至少两个修饰反应中的固相偶联核苷产生文库多样性，预期的文库和化合物包括各种2-C取代的嘌呤，3-脱氧/氮杂-6-取代的嘌呤， 取代的2-硫代腺嘌呤，2-氨基-6,8-二取代嘌呤，2,8-二取代鸟苷，6-取代嘌呤，2,6-二取代腺苷和6,8-二取代腺苷。 特别优选的化合物包括使用预期的文库产生的核苷类似物，其可用于治疗各种病症，特别是病毒感染和肿瘤疾病。

公开(公告)号：WO2007121481A2

公开(公告)日：2007-10-25

申请号：PCT/US2007066894

申请日：2007-04-18

Applicant: ARDEA BIOSCIENCES INC ,  KOH YUNG-HYO ,  HONG ZHI ,  VERNIER JEAN-MICHEL ,  CHOW SUETYING ,  YAN SHUNGI

Inventor： KOH YUNG-HYO ,  HONG ZHI ,  VERNIER JEAN-MICHEL ,  CHOW SUETYING ,  YAN SHUNGI

IPC: A61K31/44 ,  C07D211/84

CPC classification number: C07D213/76

Abstract: This invention concerns ~N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N'-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract translation: 本发明涉及〜N-（邻苯基氨基二氢吡啶基）磺酰胺和N-（邻苯基氨基二氢吡啶基），N' - 烷基磺酰胺，它们是MEK的抑制剂，可用于治疗癌症和其它过度增殖性疾病。

公开(公告)号：WO2004080466A1

公开(公告)日：2004-09-23

申请号：PCT/US2003/006992

申请日：2003-03-07

Applicant: RIBAPHARM INC. ,  GIRARDET, Jean-Luc ,  KOH, Yung-hyo ,  AN, Haoyun ,  HONG, Zhi

Inventor： GIRARDET, Jean-Luc ,  KOH, Yung-hyo ,  AN, Haoyun ,  HONG, Zhi

IPC: A61K31/522

CPC classification number: C07D487/04 ,  C07F9/6561 ,  C07H19/14 ,  C07H19/16 ,  C07H19/173 ,  C07H19/20 ,  C07H19/23

Abstract: Cytidine analogs, their prodrugs and/or metabolites are employed as pharmaceutically active compounds for treatment of diseases responsive to such compounds. Particularly preferred diseases include viral diseases (e.g., HCV infection) and neoplasms.

Abstract translation: 胞苷类似物，其前药和/或代谢物被用作药物活性化合物，用于治疗对这些化合物有反应的疾病。 特别优选的疾病包括病毒性疾病（例如HCV感染）和赘生物。

公开(公告)号：WO2008058285A3

公开(公告)日：2008-05-15

申请号：PCT/US2007/084342

申请日：2007-11-09

Applicant: ARDEA BIOSCIENCES, INC. ,  GIRARDET, Jean-luc ,  HONG, Zhi ,  SHAW, Stephanie ,  KOH, Yung-hyo

Inventor： GIRARDET, Jean-luc ,  HONG, Zhi ,  SHAW, Stephanie ,  KOH, Yung-hyo

IPC: C07D495/04 ,  C07D237/28 ,  A61K31/519 ,  A61K31/517 ,  A61P31/18

Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula (I) where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

公开(公告)号：WO2007121481A8

公开(公告)日：2008-10-16

申请号：PCT/US2007066894

申请日：2007-04-18

Applicant: ARDEA BIOSCIENCES INC ,  YAN SHUNQI ,  VERNIER JEAN-MICHEL ,  HONG ZHI ,  CHOW SUETYING ,  KOH YUNG-HYO

Inventor： YAN SHUNQI ,  VERNIER JEAN-MICHEL ,  HONG ZHI ,  CHOW SUETYING ,  KOH YUNG-HYO

IPC: A61K31/44 ,  C07D211/48

CPC classification number: C07D213/76

Abstract: This invention concerns ~N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N'-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract translation: 本发明涉及〜N-（邻苯基氨基二氢吡啶基）磺酰胺和N-（邻苯基氨基二氢吡啶基），N' - 烷基磺酰胺，它们是MEK的抑制剂，可用于治疗癌症和其它过度增生性疾病。

公开(公告)号：WO2008089459A1

公开(公告)日：2008-07-24

申请号：PCT/US2008/051518

申请日：2008-01-18

Applicant: ARDEA BIOSCIENCES, INC. ,  VERNIER, Jean-michel ,  MADERNA, Andreas ,  KOH, Yung-hyo ,  HONG, Zhi

Inventor： VERNIER, Jean-michel ,  MADERNA, Andreas ,  KOH, Yung-hyo ,  HONG, Zhi

IPC: C07D231/56 ,  C07D235/14 ,  C07D239/74 ,  C07D261/20 ,  C07D471/04 ,  A61P35/00 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4353

CPC classification number: C07D231/56 ,  C07D235/14 ,  C07D239/74 ,  C07D261/20 ,  C07D471/04

Abstract: This invention concerns to N-(2-aylamino) aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及作为MEK抑制剂的N-（2-芳基氨基）芳基磺酰胺，使用这些化合物治疗过度增殖性疾病的方法以及含有这些化合物的药物组合物。