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公开(公告)号：US06228868B1
公开(公告)日：2001-05-08
申请号：US09360463
申请日：1999-07-23
申请人： Stephen L. Gwaltney, II , Hwan-Soo Jae , Douglas M. Kalvin , Gang Liu , Hing L. Sham , Qun Li , Akiyo K. Claiborne , Le Wang , Kenneth J. Barr , Keith W. Woods
发明人： Stephen L. Gwaltney, II , Hwan-Soo Jae , Douglas M. Kalvin , Gang Liu , Hing L. Sham , Qun Li , Akiyo K. Claiborne , Le Wang , Kenneth J. Barr , Keith W. Woods
IPC分类号： A61K31421
CPC分类号： C07D413/04 , C07D263/14
摘要： Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.
摘要翻译： 具有式Iare的化合物可用于治疗癌症。 还公开了包含式I化合物的药物组合物和治疗哺乳动物癌症的方法。
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公开(公告)号：US06204293B1
公开(公告)日：2001-03-20
申请号：US09073807
申请日：1998-05-07
申请人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
发明人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
IPC分类号： C07C26302
CPC分类号： C07C237/36 , C07B2200/07 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D249/08 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08 , C07F9/5333
摘要： Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5 —, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译： 具有式的化合物或其药学上可接受的盐，其中R 1是（a）氢，（b）低级烷基，（c）烯基，（d）烷氧基，（e）硫代烷氧基，（f）卤素，（g）卤代烷基，（h） 芳基-L2-和（i）杂环-L2-; R2选自（b）-C（O）NH-CH（R14）-C（O）OR15，（d）-C（O）NH-CH（R14）-C（O）NHSO2R16，（e） C（O）NH-CH（R 14） - 四唑基，（f）-C（O）NH-杂环基和（g）-C（O）NH-CH（R 14）-C（O）NR 17 R 18; R3是杂环，芳基，取代或未取代的环烷基; R4是氢，低级烷基，卤代烷基，卤素，芳基，芳基烷基，杂环或（杂环）烷基; （a）-L4-N（R5）-L5-，（b）-L4-O-L5-，（c）-L4-S（O）n-L5-（d） - L4-L6-C（W）-N（R5）-L5-，（e）-L4-L6-S（O）mN（R5）-L5 - ，（f）-L4-N（R5）-C W）-L7-L5 - ，（g）-L4-N（R5）-S（O）p-L7-L5-，（h）任选取代的亚烷基，（i）任选取代的亚烯基，和（j） 亚炔基是蛋白质异戊二烯转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
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公开(公告)号：US06310095B1
公开(公告)日：2001-10-30
申请号：US09073794
申请日：1998-05-07
申请人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorenson , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang
发明人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorenson , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang
IPC分类号： A61K31192
CPC分类号： C07D207/08 , C07B2200/07 , C07C237/36 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D249/08 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08 , C07F9/5333
摘要： Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译： 具有式的化合物或其药学上可接受的盐，其中R 1是（a）氢，（b）低级烷基，（c）烯基，（d）烷氧基，（e）硫代烷氧基，（f）卤素，（g）卤代烷基，（h） 芳基-L2-和（i）杂环-L2-; R 2选自（a）（b）-C（O）NH-CH（R 14）-C（O）OR 15，（d）-C（O）NH-CH（R 14）-C（O）NHSO 2 R 16 e）-C（O）NH-CH（R14） - 四唑基，（f）-C（O）NH-杂环基和（g）-C（O）NH-CH（R14）-C（O）NR17R18; R 3是取代或未取代的杂环或芳基，取代或未取代的环烷基或环烯基，和-P（W）RR 3 R R 3'; R4是氢，低级烷基，卤代烷基，卤素，芳基，芳基烷基，杂环或（杂环）烷基; （a）-L4-N（R5）-L5-，（b）-L4-O-L5-，（c）-L4-S（O）n-L5-（d） - L4-L6-C（W）-N（R5）-L5-，（e）-L4-L6-S（O）mN（R5）-L5 - ，（f）-L4-N（R5）-C W）-L7-L5-，（g）-L4-N（R5）-S（O）p-L7-L5-，（h）任选取代的亚烷基，（i）任选取代的亚烯基，（j）任选取代的亚炔基 （k）共价键，（1）和（m）是蛋白质异戊二烯基转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
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公开(公告)号：US08648069B2
公开(公告)日：2014-02-11
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4192 , C07D417/14 , C07D405/14 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。 本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。
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公开(公告)号：US20090203690A1
公开(公告)日：2009-08-13
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4192 , C07D413/14 , C12N9/99 , A61P25/28 , A61P35/00
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。 本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。
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公开(公告)号：US07737159B2
公开(公告)日：2010-06-15
申请号：US11675160
申请日：2007-02-15
申请人： David D. Anderson , Bruce A. Beutel , Curt S. Cooper , Yu-Gui Gu , Mira M. Hinman , Douglas M. Kalvin , Robert F. Keyes , Xenia B. Searle , Rolf Wagner
发明人： David D. Anderson , Bruce A. Beutel , Curt S. Cooper , Yu-Gui Gu , Mira M. Hinman , Douglas M. Kalvin , Robert F. Keyes , Xenia B. Searle , Rolf Wagner
IPC分类号： A61K31/44 , C07D515/02
CPC分类号： C07D513/04 , C07D207/12 , C07D207/16 , C07D239/48 , C07D277/36 , C07D471/04
摘要： Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates in the processes, compositions containing the compounds, and methods of using the compounds are disclosed.
摘要翻译： 公开了具有式（I）的具有式（I）的细菌蛋白质合成抑制化合物及其前体药物的前体药物，其制备方法，含该化合物的组合物，使用该化合物的方法。
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公开(公告)号：US07196200B2
公开(公告)日：2007-03-27
申请号：US10762002
申请日：2004-01-21
申请人： David D. Anderson , Bruce A. Beutel , Curt S. Cooper , Yu-Gui Gu , Mira M. Hinman , Douglas M. Kalvin , Robert F. Keyes , Xenia B. Searle , Rolf Wagner
发明人： David D. Anderson , Bruce A. Beutel , Curt S. Cooper , Yu-Gui Gu , Mira M. Hinman , Douglas M. Kalvin , Robert F. Keyes , Xenia B. Searle , Rolf Wagner
IPC分类号： C07D277/60 , A01N43/78
CPC分类号： C07D513/04 , C07D207/12 , C07D207/16 , C07D239/48 , C07D277/36 , C07D471/04
摘要： Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates in the processes, compositions containing the compounds, and methods of using the compounds are disclosed.
摘要翻译： 具有式（I）的细菌蛋白质合成抑制化合物
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公开(公告)号：US06777535B1
公开(公告)日：2004-08-17
申请号：US09703233
申请日：2000-10-31
IPC分类号： C07K700
摘要： N-Alkylated peptides of formula (I) Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11 (I), are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要翻译： 式（I）的N-烷基化肽可用于抑制血管发生。 还公开了血管生成抑制组合物和抑制哺乳动物血管发生的方法。
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公开(公告)号：US06753408B1
公开(公告)日：2004-06-22
申请号：US09718591
申请日：2000-11-22
IPC分类号： C07K700
CPC分类号： C07K7/06
摘要： Peptides of formula (I) Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11 (I), are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要翻译： 式（I）的肽可用于抑制血管发生。 还公开了血管生成抑制组合物和抑制哺乳动物血管发生的方法。
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公开(公告)号：US06716963B1
公开(公告)日：2004-04-06
申请号：US09447226
申请日：1999-11-22
IPC分类号： C07K700
CPC分类号： C07K7/06
摘要： Peptides having the formula: A0-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10 wherein A0 is selected from hydrogen or an acyl group; A10 is a hydroxyl group or an amino acid amide; and A1, A2, A3, A4, A5, A6, A7, A8, and A9 are amino acyl residues as defined herein.
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