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    Process for preparing azacycloalkanoylaminothiazoles
    2.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号：US06639074B2

    公开(公告)日：2003-10-28

    申请号：US10100129

    申请日：2002-03-18

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    IPC分类号： C07D47100

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2 R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素 ，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

    Process for preparing azacycloalkanoylaminothiazoles
    3.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号：US06414156B2

    公开(公告)日：2002-07-02

    申请号：US09746060

    申请日：2000-12-22

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    IPC分类号： C07D41714

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2，R 3， R4和R5各自独立地为氢，烷基，芳基或杂芳基; R6和R7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R8为氢，烷基，芳基，杂芳基，CONR9R10，COR11或COOR12; R9，R10，R11和R12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

    Process for preparing arylacetylaminothiazoles
    4.
    发明授权
    Process for preparing arylacetylaminothiazoles 有权
    制备芳基乙酰氨基噻唑的方法

    公开(公告)号：US06613911B2

    公开(公告)日：2003-09-02

    申请号：US10067723

    申请日：2002-02-05

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Joseph E. Sundeen ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Joseph E. Sundeen ,  Rulin Zhao

    IPC分类号： C07D41712

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: or a pharmnaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-芳基乙酰氨基噻唑化合物的新的，有效的方法：或其药物上可接受的盐，其中：R1，R2，R4，R5，R6，R8， R9，R12和R13各自独立地为氢，烷基，芳基或杂芳基; R3，R7，R10和R11各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; 而X是CH或N，它们是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还涉及制备甲酰芳基乙酸酯和甲酰芳基乙酸的新方法。

    Process for preparing arylacetylaminothiazoles
    5.
    发明授权
    Process for preparing arylacetylaminothiazoles 有权
    制备芳基乙酰氨基噻唑的方法

    公开(公告)号：US06392053B2

    公开(公告)日：2002-05-21

    申请号：US09746059

    申请日：2000-12-22

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Joseph E. Sundeen ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Joseph E. Sundeen ,  Rulin Zhao

    IPC分类号： C07D41712

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-芳基乙酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R1，R2，R4，R5，R6，R8，R9， R 12和R 13各自独立地为氢，烷基，芳基或杂芳基; R 3，R 7，R 10和R 11各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; 而X是CH或N，它们是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还涉及制备甲酰芳基乙酸酯和甲酰芳基乙酸的新方法。

    Monobactam hydrazides containing catechol sulfonic acid groups
    9.
    发明授权
    Monobactam hydrazides containing catechol sulfonic acid groups 失效
    含有邻苯二酚磺酸基团的单链酰肼

    公开(公告)号：US5077432A

    公开(公告)日：1991-12-31

    申请号：US651871

    申请日：1991-02-07

    申请人： Joseph E. Sundeen ,  Robert Zahler ,  Stefan Jendrzejewski

    发明人： Joseph E. Sundeen ,  Robert Zahler ,  Stefan Jendrzejewski

    IPC分类号： C07C309/51 ,  C07D417/12

    CPC分类号： C07D417/12 ,  C07C309/51

    摘要： Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl or R.sub.3 and R.sub.4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring and Y, and Y.sub.2 are either hydrogen or hydroxy but are not the same; are useful chemical intermediates for the preparation of .beta.-lactam antibiotics.

    摘要翻译： 具有式“IMAGE”的化合物及其药学上可接受的盐，其中R 3和R 4相同或不同，并且各自为氢或烷基或R 3和R 4与它们所连接的氮原子一起形成1,2-二氮环丁烷 ，1,2-二氮杂环戊烷，1,2-二氮杂环己烷或1,2-二氮杂环庚烷环，Y和Y2分别是氢或羟基，但不相同; 是制备β-内酰胺抗生素的有用化学中间体。

    Inhibitors of mammalian collagenase
    10.
    发明授权
    Inhibitors of mammalian collagenase 失效
    哺乳动物胶原酶抑制剂

    公开(公告)号：US4382081A

    公开(公告)日：1983-05-03

    申请号：US273142

    申请日：1981-06-12

    申请人： Joseph E. Sundeen ,  Tamara Dejneka

    发明人： Joseph E. Sundeen ,  Tamara Dejneka

    IPC分类号： C12N9/99 ,  A61K31/195 ,  A61K38/00 ,  A61K38/55 ,  C07C55/02 ,  C07C67/00 ,  C07C313/00 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C327/20 ,  C07C327/32 ,  C07K5/02 ,  C07K5/04 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K14/81 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/1008 ,  C07C323/52 ,  C07C323/56 ,  C07C327/00 ,  C07C55/02 ,  C07K5/06026 ,  C07K5/0806

    摘要： Mammalian collagenase is inhibited by compounds of the formula ##STR1## or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; ##STR2## R.sub.4 is hydrogen, methyl, ethyl, or ##STR3## R.sub.5 and R.sub.6 are each independently selected as --OCH.sub.3 or --OCH.sub.2 CH.sub.3 or are combined as --OCH.sub.2 CH.sub.2 O-- or --O--(CH.sub.2)--O--;R.sub.7 and R.sub.8 are each independently selected as hydrogen, methyl or ethyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --;R.sub.9 is hydrogen, methyl, ethyl ##STR4## m is an integer from 0 to 7; p is an integer from 1 to 3; AA.sub.n is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3;when p is 1, AA.sub.n is AA.sub.1 ;when p is 2, AA.sub.n is AA.sub.1 --AA.sub.2 ;when p is 3, AA.sub.n is AA.sub.1 --AA.sub.2 --AA.sub.3 ;AA.sub.1 is glycine or alanine;AA.sub.2 is glycine or alanine;AA.sub.3 is leucine, glutamine or isoleucine.A method of reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to the mammal an effective amount of a compound having the above formula is within the scope of the invention.

    摘要翻译： 哺乳动物胶原酶被下式化合物或其盐抑制，其中R是氢，2-10个碳原子的烷酰基或芳基羰基; R1为3〜8个碳原子的烷基，3〜7个碳原子的环烷基，芳基或芳基烷基; R 4是氢，甲基，乙基或者R 5，R 6和R 6各自独立地选自-OCH 3或-OCH 2 CH 3，或者作为-OCH 2 CH 2 O-或-O - （CH 2）-O-; R 7和R 8各自独立地选自氢，甲基或乙基，或者作为 - （CH 2）4 - ， - （CH 2）5 - 或-CH 2 CH 2 -O-CH 2 CH 2 - R9是氢，甲基，乙基，是0至7的整数; p是1至3的整数; AAn是一至三个氨基酸的氨基酸链; n为1或1,2或1，2，3; 当p为1时，AAn为AA1; 当p为2时，AAn为AA1-AA2; 当p为3时，AAn为AA1-AA2-AA3; AA1是甘氨酸或丙氨酸; AA2是甘氨酸或丙氨酸; AA3是亮氨酸，谷氨酰胺或异亮氨酸。 减少有需要的哺乳动物宿主中哺乳动物胶原酶的不利影响的方法，其包括向哺乳动物施用有效量的具有上式的化合物在本发明的范围内。