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21. 发明申请

WO2002100844A2 HIV PROTEASE INHIBITORS, COMPOSITIONS CONTAINING THE SAME, THEIR PHARMACEUTICAL USES AND MATERIALS FOR THEIR SYNTHESIS 审中-公开
标题翻译： HIV蛋白酶抑制剂，含有它们的组合物，它们的药物用途和材料合成
公开(公告)号：WO2002100844A2
公开(公告)日：2002-12-19
申请号：PCT/US2002/018717
申请日：2002-06-11
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： CANON-KOCH, Stacie, S. , ALEXANDER, Therese, N. , BARVIAN, Mark , BOLTON, Gary , BOYER, Fredrick, E. , BURKE, Benjamin, J. , HOLLER, Tod , JEWELL, Tanya, M. , PRASAD JOSYULA, Vara , KUCERA, David, J. , LINTON, Maria, A. , MACHAK, Jeff , MITCHELL, Lennert, J. , MURPHY, Sean, T. , REICH, Siegfried, H. , SKALITZKY, Donald, J. , TATLOCK, John, H. , VARNEY, Michael, D. , VIRGIL, Scott, C. , WEBBER, Stephen, E. , WORLAND, Stephen, T. , MELNICK, Michael
IPC分类号： C07D277/00
CPC分类号： C07D231/12 , A61K31/426 , A61K31/427 , C07D207/09 , C07D207/16 , C07D213/38 , C07D217/26 , C07D277/06 , C07D277/60 , C07D295/13 , C07D307/52 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/08
摘要： Compounds of Formula (I), where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
摘要翻译：公开了式（I）化合物，其中式变量如本文所定义，其有利地抑制或阻断HIV蛋白酶的生物活性。这些化合物以及含有这些化合物的药物组合物可用于治疗感染HIV病毒的患者或宿主。还描述了制备这些化合物的中间体和合成方法。

22. 发明申请

WO1997011938A1 PROCESS FOR PRODUCING AMIDE DERIVATIVES AND INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：生产酰胺衍生物和中间体化合物的方法
公开(公告)号：WO1997011938A1
公开(公告)日：1997-04-03
申请号：PCT/JP1996002757
申请日：1996-09-24
申请人： JAPAN TOBACCO INC. , AGOURON PHARMACEUTICALS, INC. , INABA, Takashi , YAMADA, Yasuki , SHANLEY, James , DEASON, Michael
发明人： JAPAN TOBACCO INC. , AGOURON PHARMACEUTICALS, INC.
IPC分类号： C07C323/25
CPC分类号： C07D317/28 , C07C319/20 , C07D319/20 , C07D321/06 , C07C323/25
摘要： A process for producing amide derivatives represented by general formula (XV) or enantiomers thereof, novel intermediate compounds useful for producing these compounds, etc., and a process for producing the same, wherein each symbol is as defined in the specification. Compared with the conventional processes, the above process can be very easily effected and enables an efficient production of the compounds (XV), i.e., those involving the compounds (XVI) having an HIV protease inhibitory effect in high yields. The novel intermediates are highly advantageous as intermediates for producing not only the above compounds (XVI) but also those which are useful as an X-ray contrast medium, etc.
摘要翻译：一种制备由通式（ⅩⅤ）表示的酰胺衍生物或其对映异构体的方法，可用于制备这些化合物的新型中间体化合物及其制备方法，其中各符号如说明书中所定义。与常规方法相比，上述方法可以非常容易地实现，并且能够以高产率有效地生成化合物（XV），即涉及具有HIV蛋白酶抑制作用的化合物（ⅩⅥ）的那些。新颖的中间体作为不仅产生上述化合物（XVI）的中间体而且作为用作X射线造影剂等的那些是非常有利的。

23. 发明申请

WO1996003406A1 COMPOUNDS USEFUL AS ANTIPROLIFERATIVE AGENTS AND GARFT INHIBITORS 审中-公开
标题翻译：化合物作为抗增生剂和甘油抑制剂有用
公开(公告)号：WO1996003406A1
公开(公告)日：1996-02-08
申请号：PCT/US1995009519
申请日：1995-07-28
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： AGOURON PHARMACEUTICALS, INC. , VARNEY, Michael, D. , ROMINES, William, H.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D333/38 , C07D513/04
摘要： Compounds of formula (I), which are in equilibrium with their 4-hydroxy tautomers and are in the form of diastereomeric mixtures, and their pharmaceutically acceptable salts are potent GARFT inhibitors. A is S, CH2 or Se; Z is a substituted or unsubstituted C1-C3 alkyl, C2-C3 alkenyl, C2-C3 alkynyl or amino group, or S or O; X is a substituted or unsubstituted C1-C6 alkyl group; a substituted or unsubstituted C2-C6 alkynyl group; a substituted or unsubstituted C2-C6 alkynyl group; -C(O)E, wherein E is hydrogen, a substituted or unsubstituted C1-C3 alkyl group, a substituted or unsubstituted C2-C3 alkenyl group, a substituted or unsubstituted C2-C3 alkynyl group, a substituted or unsubstituted OC1-C3 alkoxy group, or NR10R11, wherein R10 and R11 are independently selected from hydrogen, substituted and unsubstituted C1-C3 alkyl groups, substituted and unsubstituted C2-C3 alkenyl groups, substituted and unsubstituted C2-C3 alkynyl groups; NR10R11, wherein R10 and R11 are independently defined as set forth above; hydroxyl; nitro; SR12, wherein R12 is hydrogen, a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C2-C6 alkenyl group, or a substituted or unsubstituted C2-C6 alkynyl group; cyano; or a substituted or unsubstituted C1-C3 alkoxy group; and R1 and R2 are independently hydrogen or a moiety that forms with the attached CO2 a readily hydrolyzable ester group. These compounds and their salts are useful as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents. The invention also relates to compounds useful as intermediates for preparing such compounds, and to their synthesis.
摘要翻译：与其4-羟基互变异构体平衡并且呈非对映体混合物形式的式（I）化合物及其药学上可接受的盐是有效的GARFT抑制剂。 A是S，CH 2或Se; Z是取代或未取代的C 1 -C 3烷基，C 2 -C 3烯基，C 2 -C 3炔基或氨基，或S或O; X是取代或未取代的C 1 -C 6烷基; 取代或未取代的C 2 -C 6炔基; 取代或未取代的C 2 -C 6炔基; -C（O）E，其中E为氢，取代或未取代的C1-C3烷基，取代或未取代的C2-C3烯基，取代或未取代的C2-C3炔基，取代或未取代的OC1-C3烷氧基基团或NR 10 R 11，其中R 10和R 11独立地选自氢，取代和未取代的C 1 -C 3烷基，取代和未取代的C 2 -C 3烯基，取代和未取代的C 2 -C 3炔基; NR10R11，其中R10和R11独立地定义如上所述; 羟; 硝基; SR12，其中R12是氢，取代或未取代的C1-C6烷基，取代或未取代的C2-C6烯基或取代或未取代的C2-C6炔基; 氰基; 或取代或未取代的C 1 -C 3烷氧基; 并且R 1和R 2独立地为氢或与所连接的CO 2形成易于水解的酯基的部分。这些化合物及其盐可用作抗增殖剂。本发明还涉及使用诸如GARFT抑制剂或抗增殖剂的化合物的药物组合物和方法。本发明还涉及可用作制备这些化合物的中间体的化合物及其合成。

24. 发明申请

WO1994015906A1 HIV PROTEASE INHIBITORS AND THEIR PREPARATION 审中-公开
标题翻译：艾滋病病毒蛋白酶抑制剂及其制备
公开(公告)号：WO1994015906A1
公开(公告)日：1994-07-21
申请号：PCT/US1994000420
申请日：1994-01-18
申请人： AGOURON PHARMACEUTICALS, INC. , REICH, Siegfried, H. , PINO, Mark, J. , NGUYEN, Dzuy, T. , TRIPPE, Anthony, J.
发明人： AGOURON PHARMACEUTICALS, INC.
IPC分类号： C07C233/65
CPC分类号： C07D213/40 , A61K38/00 , C07C235/42 , C07C235/66 , C07C237/30 , C07C323/60 , C07C323/62 , C07C323/63 , C07C2601/08 , C07C2602/24 , C07C2602/28 , C07D207/16 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/68 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/08 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D217/26 , C07D233/64 , C07D263/14 , C07D295/192 , C07D307/14 , C07D307/83 , C07D311/76 , C07D319/06 , C07D327/02 , C07K5/0205
摘要： HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
摘要翻译：可通过化学合成获得的HIV蛋白酶抑制剂阻断HIV蛋白酶的生物学活性，导致HIV病毒的复制终止。因此，这些化合物以及含有这些化合物和可能的其它抗病毒剂作为成分的药物组合物适用于已知引起AIDS的HIV病毒的治疗。

25. 发明申请

WO1991012718A1 ENHANCED CRYOPRESERVATION WITH THERMAL HYSTERESIS PEPTIDE 审中-公开
标题翻译：用热滞留肽进行增强CRYOPRESERVATION
公开(公告)号：WO1991012718A1
公开(公告)日：1991-09-05
申请号：PCT/US1991001413
申请日：1991-03-01
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： AGOURON PHARMACEUTICALS, INC. , CARPENTER, John, F.
IPC分类号： A01N01/00
CPC分类号： A01N1/0221 , A01N1/02 , C07K14/46 , C12N1/04
摘要： A composition is provided for enhancing survival of biological materials during freezing and thawing. The composition includes at least one cryoprotectant and a thermal hysteresis peptide in an amount effective for enhancing the viability of the biological material. A method of enhancing survival of biological materials during freezing and thawing is also provided. A method for preserving the functional integrity of membrane enclosed of bound material during freeze-drying is also provided.
摘要翻译：提供了用于在冷冻和解冻期间增强生物材料的存活的组合物。该组合物包含至少一种有效提高生物材料生存能力的冷冻保护剂和热滞后肽。还提供了一种在冷冻和解冻过程中提高生物材料生存的方法。还提供了一种在冷冻干燥期间保持封闭的结合材料的膜的功能完整性的方法。

26. 发明申请

WO2003004467A2 THIAZOLE BENZAMIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING CELL PROLIFERATION, AND METHODS FOR THEIR USE 审中-公开
标题翻译：用于抑制细胞增殖的噻唑衍生物和药物组合物及其使用方法
公开(公告)号：WO2003004467A2
公开(公告)日：2003-01-16
申请号：PCT/US2002/021280
申请日：2002-07-05
申请人： AGOURON PHARMACEUTICALS, INC. , CHU, Shao, Song , ALEGRIA, Larry, Andrew , BLECKMAN, Ted, Michael , CHONG, Wesley, K., M. , DUVADIE, Rohit, K. , LI, Lin , REICH, Siegfried, H. , ROMINES, William, H. , WALLACE, Michael, B. , YANG, Yi
发明人： CHU, Shao, Song , ALEGRIA, Larry, Andrew , BLECKMAN, Ted, Michael , CHONG, Wesley, K., M. , DUVADIE, Rohit, K. , LI, Lin , REICH, Siegfried, H. , ROMINES, William, H. , WALLACE, Michael, B. , YANG, Yi
IPC分类号： C07D
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/12 , C07D491/10
摘要： Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
摘要翻译：描述了具有单/二取代苯甲酰胺的氨基噻唑化合物由式（I）表示，并且描述了其药学上可接受的盐，药学上可接受的前药，药学活性代谢物和所述代谢物的药学上可接受的盐。这些药物调节和/或抑制蛋白激酶的细胞增殖和活性，并且可用作治疗恶性肿瘤和其它疾病的药物。

27. 发明申请

WO1998017643A1 HETEROARYL SUCCINAMIDES AND THEIR USE AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： HETEROARYL SUCCINAMIDES及其作为金属蛋白酶抑制剂使用
公开(公告)号：WO1998017643A1
公开(公告)日：1998-04-30
申请号：PCT/US1997017809
申请日：1997-10-06
申请人： AGOURON PHARMACEUTICALS, INC. , SYNTEX (U.S.A.) INC.
发明人： AGOURON PHARMACEUTICALS, INC. , SYNTEX (U.S.A.) INC. , BENDER, Steven, L. , CASTELHANO, Arlindo, L. , CHONG, Wesley, K., M. , ABREO, Melwyn, A. , BILLEDEAU, Roland, J. , CHEN, Jian, Jeffrey , DEAL, Judith, G.
IPC分类号： C07D207/327
CPC分类号： C07D207/327 , A61K38/00 , C07D207/337 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/54 , C07D333/24 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D487/08 , C07K5/06104 , C07K5/06113
摘要： The present invention is directed to compound of formula (I), wherein R1, R2, R3, R4, R5, X, Y and (Ia) are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，X，Y和（Ia）如本文所定义。这些化合物可用于通过使金属蛋白酶与有效量的本发明化合物接触来抑制金属蛋白酶的活性。

28. 发明申请

WO1996016027A1 MATRIX METALLOPROTEASE INHIBITORS 审中-公开
标题翻译： MATRIX METALLOPROTEASE抑制剂
公开(公告)号：WO1996016027A1
公开(公告)日：1996-05-30
申请号：PCT/US1995015530
申请日：1995-11-21
申请人： SYNTEX (U.S.A.) INC. , AGOURON PHARMACEUTICALS, INC.
发明人： SYNTEX (U.S.A.) INC. , AGOURON PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , BENDER, Steven, L. , DEAL, Judith, G. , HORNE, Stephen , LIAK, Teng, J. , YUAN, Zhengyu
IPC分类号： C07C259/06
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/58 , C07F9/60 , C07F9/65583
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.
摘要翻译：式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶，例如溶基质溶解素，明胶酶，基质溶素和胶原酶，并且可用于治疗通过抑制这种基质金属蛋白酶而减轻疾病的哺乳动物。

29. 发明申请

WO1995032185A1 N-(3-AMINO-2-HYDROXYBUTYL)SULPHONAMIDE DERIVATIVES AS HIV PROTEASE INHIBITORS 审中-公开
标题翻译： N-（3-氨基-2-羟基丁基）磺酰胺衍生物作为HIV蛋白酶抑制剂
公开(公告)号：WO1995032185A1
公开(公告)日：1995-11-30
申请号：PCT/US1995006866
申请日：1995-05-23
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： AGOURON PHARMACEUTICALS, INC. , KALISH, Vincent, J.
IPC分类号： C07C323/49
CPC分类号： C07C323/49
摘要： HIV protease inhibitors of formula (1), in which Q1 to Q8, E, and Y are as defined in Claim 1, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
摘要翻译：式（1）的HIV蛋白酶抑制剂，其中Q1至Q8，E和Y如权利要求1所定义，可通过化学合成获得，抑制或阻断HIV蛋白酶的生物活性，导致HIV病毒的复制终止。这些化合物以及含有这些化合物和任选的其它抗病毒剂作为活性成分的药物组合物适用于治疗已知导致AIDS的HIV病毒感染的患者或宿主。

30. 发明申请

WO1994013295A1 ANTIPROLIFERATIVE SUBSTITUTED 5-THIAPYRIMIDINONE AND 5-SELENOPYRIMIDINONE COMPOUNDS 审中-公开
标题翻译：抗生素替代的5-巯基嘧啶酮和5-巯基嘧啶酮化合物
公开(公告)号：WO1994013295A1
公开(公告)日：1994-06-23
申请号：PCT/US1993011795
申请日：1993-12-10
申请人： AGOURON PHARMACEUTICALS, INC. , DEAL, Judith, G. , VARNEY, Michael, D. , ROMINES, William, H. , PALMER, Cynthia, L.
发明人： AGOURON PHARMACEUTICALS, INC.
IPC分类号： A61K31/505
CPC分类号： C07D239/56 , C07D409/12
摘要： Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.
摘要翻译：发现5-硫杂和5-硒代嘧啶酮的新型衍生物可抑制甘氨酰胺核糖核苷酸甲酰转移酶（GARFT）和氨基咪唑甲酰胺核糖核苷酸甲酰转移酶（AICARFT）。还公开了这些化合物的新型中间体。还公开了制备这些化合物的新方法，以及使用该化合物作为抗增殖剂的方法和组合物。

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