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公开(公告)号：US07179918B2
公开(公告)日：2007-02-20
申请号：US10166979
申请日：2002-06-11
申请人： Stacie S. Canan Koch , Therese N. Alexander , Benjamin J. Burke , Tanya M. Jewell , David J. Kucera , Maria Angelica Linton , Lennert J. Mitchell, Jr. , Siegfried H. Reich , Donald J. Skalitzky , John H. Tatlock , Michael D. Varney , Scott C. Virgil , Stephen E. Webber , Stephen T. Worland , Mark Barvian , Gary Bolton , Frederick Earl Boyer, Jr. , Jeffrey J. Machak , Tod Holler , Sean T. Murphy , Michael Melnick , Vara Prasad Josyula
发明人： Stacie S. Canan Koch , Therese N. Alexander , Benjamin J. Burke , Tanya M. Jewell , David J. Kucera , Maria Angelica Linton , Lennert J. Mitchell, Jr. , Siegfried H. Reich , Donald J. Skalitzky , John H. Tatlock , Michael D. Varney , Scott C. Virgil , Stephen E. Webber , Stephen T. Worland , Mark Barvian , Gary Bolton , Frederick Earl Boyer, Jr. , Jeffrey J. Machak , Tod Holler , Sean T. Murphy , Michael Melnick , Vara Prasad Josyula
IPC分类号： C07D207/16 , C07D221/02
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 the formula: 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.
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2.发明授权HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 失效HIV蛋白酶抑制剂，含有它们的组合物，它们的药物用途和用于合成的材料公开(公告)号：US06953858B2
公开(公告)日：2005-10-11
申请号：US10166957
申请日：2002-06-11
申请人： Stacie S. Canan Koch , Therese N. Alexander , Mark Barvian , Gary Bolton , Frederick Earl Boyer, Jr. , Benjamin J. Burke , Tod Holler , Tanya M. Jewell , Vara Prasad Josyula , David J. Kucera , Maria Angelica Linton , Jeffrey J. Machak , Lennert J. Mitchell, Jr. , Sean T. Murphy , Siegfried H. Reich , Donald J. Skalitzky , John H. Tatlock , Michael D. Varney , Scott C. Virgil , Stephen E. Webber , Stephen T. Worland , Michael Melnick
发明人： Stacie S. Canan Koch , Therese N. Alexander , Mark Barvian , Gary Bolton , Frederick Earl Boyer, Jr. , Benjamin J. Burke , Tod Holler , Tanya M. Jewell , Vara Prasad Josyula , David J. Kucera , Maria Angelica Linton , Jeffrey J. Machak , Lennert J. Mitchell, Jr. , Sean T. Murphy , Siegfried H. Reich , Donald J. Skalitzky , John H. Tatlock , Michael D. Varney , Scott C. Virgil , Stephen E. Webber , Stephen T. Worland , Michael Melnick
IPC分类号： C07D277/04 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/472 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K38/04 , A61K45/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P37/02 , A61P43/00 , C07D207/09 , C07D207/16 , C07D207/24 , C07D209/52 , C07D213/38 , C07D217/26 , C07D231/12 , C07D263/04 , C07D263/06 , C07D277/00 , C07D277/06 , C07D277/20 , C07D277/28 , C07D277/32 , C07D277/38 , C07D277/60 , C07D295/13 , C07D307/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/08 , C07K5/04
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 the formula: 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： 公开了下式的化合物：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。
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公开(公告)号：US5885996A
公开(公告)日：1999-03-23
申请号：US923117
申请日：1997-09-04
IPC分类号： A61K31/505 , A61K31/517 , A61P31/04 , A61P31/10 , A61P35/00 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/93 , C07D239/95 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12 , A61K31/54 , C07D403/02
CPC分类号： C07D401/12 , C07D239/90 , C07D239/93 , C07D239/95 , C07D403/06 , C07D403/12 , C07D417/12 , Y10S514/895 , Y10S514/896 , Y10S514/898
摘要： Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
摘要翻译： 显示抗增殖活性的喹唑啉化合物，例如抗肿瘤活性，制备这些化合物的方法，含有这些化合物的药物组合物，以及这些化合物的用途。 这些化合物抑制细菌，酵母和真菌等高等生物和微生物细胞的生长和增殖。 优选的喹唑啉化合物能够抑制胸苷酸合酶的酶。 由抑制酶胸苷酸合酶导致的效果包括上述讨论。
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公开(公告)号：US5707992A
公开(公告)日：1998-01-13
申请号：US418415
申请日：1995-04-07
IPC分类号： A61K31/505 , A61K31/517 , A61P31/04 , A61P31/10 , A61P35/00 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/93 , C07D239/95 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12
CPC分类号： C07D401/12 , C07D239/90 , C07D239/93 , C07D239/95 , C07D403/06 , C07D403/12 , C07D417/12 , Y10S514/895 , Y10S514/896 , Y10S514/898
摘要： Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
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公开(公告)号：US5430148A
公开(公告)日：1995-07-04
申请号：US861030
申请日：1992-03-31
IPC分类号： A61K31/505 , A61K31/517 , A61P31/04 , A61P31/10 , A61P35/00 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/93 , C07D239/95 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12
CPC分类号： C07D401/12 , C07D239/90 , C07D239/93 , C07D239/95 , C07D403/06 , C07D403/12 , C07D417/12 , Y10S514/895 , Y10S514/896 , Y10S514/898
摘要： Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
摘要翻译： 显示抗增殖活性的喹唑啉化合物，例如抗肿瘤活性，制备这些化合物的方法，含有这些化合物的药物组合物，以及这些化合物的用途。 这些化合物抑制细菌，酵母和真菌等高等生物和微生物细胞的生长和增殖。 优选的喹唑啉化合物能够抑制胸苷酸合酶的酶。 由抑制酶胸苷酸合酶导致的效果包括上述讨论。
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6.发明授权Antiproliferative substituted 5-thiapyrimidinone and 5-selenopyrimidinone compounds 失效抗增殖取代的5-硫代嘧啶酮和5-硒代嘧啶酮化合物公开(公告)号：US06323210B2
公开(公告)日：2001-11-27
申请号：US09782284
申请日：2001-02-14
IPC分类号： C07D23936
CPC分类号： C07D239/56 , C07D409/12
摘要： Novel derivatives of 5-thia- and 5-selenopyrimidinone are sound 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： 5-硫杂和5-硒代嘧啶酮的新型衍生物有效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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公开(公告)号：US5639747A
公开(公告)日：1997-06-17
申请号：US475871
申请日：1995-06-07
IPC分类号： C07D475/04 , A61K31/505 , A61K31/519 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D517/04 , C07D413/14 , A61K31/535 , A61K31/54 , C07D417/14
CPC分类号： C07D513/04
摘要： The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or 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.
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8.发明授权
公开(公告)号：US5625061A
公开(公告)日：1997-04-29
申请号：US477633
申请日：1995-06-07
IPC分类号： C07D475/04 , A61K31/505 , A61K31/519 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D517/04 , C07D403/08 , C07D403/10 , C07D403/12
CPC分类号： C07D513/04
摘要： Compounds of the invention include those of the following formula: ##STR1## In this formula, A is oxygen, sulfur or selenium; X' is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkenyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkynyl group, a substituted or unsubstituted amino group, sulfur or oxygen; Y is oxygen, sulfur or NH; B is hydrogen or a halogen; C is hydrogen, a halogen or a substituted or unsubstituted C.sub.1 -C.sub.6 alkyl group; and R.sub.6 is hydrogen or a moiety that forms with the attached CO.sub.2 a readily hydrolyzable ester group.
摘要翻译： 本发明的化合物包括下式的那些：在该式中，A是氧，硫或硒; X'是取代或未取代的C 1 -C 3烷基，取代或未取代的C 2 -C 3烯基，取代或未取代的C 2 -C 3炔基，取代或未取代的氨基，硫或氧; Y是氧，硫或NH; B是氢或卤素; C是氢，卤素或取代或未取代的C 1 -C 6烷基; 并且R 6是氢或与所连接的CO 2形成的易于水解的酯基的部分。
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公开(公告)号：US5498727A
公开(公告)日：1996-03-12
申请号：US276929
申请日：1994-07-19
申请人： Michael D. Varney , Cindy L. Palmer , Judy G. Deal
发明人： Michael D. Varney , Cindy L. Palmer , Judy G. Deal
IPC分类号： C07C255/58 , C07D209/90 , C07D209/62
CPC分类号： C07C255/58 , C07D209/90
摘要： The invention relates to a process for preparing a substituted 2-amino-benz[cd]indole of the Formula I: ##STR1## The nitro group of a substituted 1-nitro-8-cyano-naphthalene compound is reduced to an amine group to form a substituted 1-amino-8-cyano-naphthalene compound, which is cyclized to form the substituted 2-amino-benz[cd]indole. The reduction and cyclization may be effected in a one-pot procedure using a reducing agent such as stannous chloride, which generates an acid that cyclizes the reduction product. The syntheses of the 1-nitro-8-cyanonaphthalene compound and its precursors are also described.
摘要翻译： 本发明涉及制备式I的取代的2-氨基 - 苯并[cd]吲哚的方法：（I）将取代的1-硝基-8-氰基 - 萘化合物的硝基还原成 胺基以形成取代的1-氨基-8-氰基 - 萘化合物，其被环化以形成取代的2-氨基 - 苯并[cd]吲哚。 还原和环化可以在一锅法中使用还原剂如氯化亚锡进行，其产生使还原产物环化的酸。 还描述了1-硝基-8-氰基萘化合物及其前体的合成。
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公开(公告)号：US5646141A
公开(公告)日：1997-07-08
申请号：US467945
申请日：1995-06-06
IPC分类号： C07D333/70 , A61K31/505 , A61K31/522 , A61K31/54 , A61P31/00 , A61P35/00 , A61P43/00 , C07D221/00 , C07D239/00 , C07D279/00 , C07D333/38 , C07D471/04 , C07D513/04 , A61K31/535 , C07D401/14 , C07D403/14
CPC分类号： C07D471/04 , C07D333/38 , C07D513/04
摘要： Compounds of the 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: ##STR1## In the above formula, A is S, CH.sub.2 or Se, and Z, X, R.sub.1 and R.sub.2 are as defined in the specification. 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.
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：（I）在上式中，A是S， CH2或Se，Z，X，R1和R2如说明书中所定义。 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。
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