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    Crystalline (2E,4S)-4-[(N-{[(2R)-1-isopropylpiperidin-2-yI]-carbonyl}-3-methyl-L-valyl)(methyl)amino]-2,5-dimethylhex-2-enoic acid and its pharmaceutical uses
    1.
    发明申请
    Crystalline (2E,4S)-4-[(N-{[(2R)-1-isopropylpiperidin-2-yI]-carbonyl}-3-methyl-L-valyl)(methyl)amino]-2,5-dimethylhex-2-enoic acid and its pharmaceutical uses 审中-公开
    结晶（2E，4S）-4 - [（N - {[（2R）-1-异丙基哌啶-2-基] - 羰基} -3-甲基-L-缬氨酰）（甲基）氨基] -2,5-二甲基己 -2-烯酸及其药物用途

    公开(公告)号：US20060281690A1

    公开(公告)日：2006-12-14

    申请号：US11418110

    申请日：2006-05-05

    申请人： Silvio Campagna ,  Mihaela Pop

    发明人： Silvio Campagna ,  Mihaela Pop

    IPC分类号： A61K38/00

    CPC分类号： C07D211/60 ,  A61K31/445 ,  A61K38/04

    摘要： The invention relates to unsolvated and host-guest solvated crystalline forms of (2E,4S)-4-[(N-{[(2R)-1-isopropylpiperidin-2-yl]-carbonyl}-3-methyl-L-valyl)(methyl)amino]-2,5-dimethylhex-2-enoic acid, E7974, and their therapeutic uses. Pharmaceutical compositions containing crystalline forms of E7974 and a pharmaceutically acceptable carrier represent one embodiment of the invention. The invention also relates to methods for treating cancer, an inflammatory disorder, an autoimmune disorder, or a proliferative disorder as well as restenosis of blood vessels comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E7974.

    摘要翻译： 本发明涉及（2E，4S）-4 - [（N - （[（2R）-1-异丙基哌啶-2-基] - 羰基} -3-甲基-L-缬氨酰基的未溶剂化和主客体溶剂化晶体形式 ）（甲基）氨基] -2,5-二甲基己-2-烯酸E7974及其治疗用途。 含有E7974结晶形式的药物组合物和药学上可接受的载体代表本发明的一个实施方案。 本发明还涉及用于治疗癌症，炎症性疾病，自身免疫性疾病或增殖性疾病以及血管再狭窄的方法，包括向有需要的患者施用治疗有效量的结晶E7974的步骤。

    Process for the preparation of macrocyclic metalloprotease inhibitors
    2.
    发明授权
    Process for the preparation of macrocyclic metalloprotease inhibitors 失效
    制备大环金属蛋白酶抑制剂的方法

    公开(公告)号：US06307044B1

    公开(公告)日：2001-10-23

    申请号：US09329674

    申请日：1999-06-10

    申请人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    发明人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    IPC分类号： C07D27302

    CPC分类号： C07C69/007 ,  C07C43/315 ,  C07C59/58 ,  C07C235/28 ,  C07D267/00 ,  C07D273/02

    摘要： The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

    摘要翻译： 本发明涉及制备式（Xa）化合物或其药学上可接受的盐形式的方法，其中：R 1选自：被0-5个R 1a取代的C 1-5烷基， - （CH 2）r -C 3-10环烷基，被0-5个R 1a取代，和 - （CH 2）r - 被0-5个R 1a取代的芳基。式（Xa）化合物是含有抗琥珀酸酯残基的大环分子，其抑制金属蛋白酶 作为聚集蛋白聚糖酶，以及肿瘤坏死因子（TNF）的产生。 抗琥珀酸盐由爱立信选择性的甲硅烷基乙烯酮缩醛的爱尔兰克莱森重排形成。

    Process for the preparation of cyclopropylacetylene
    3.
    发明授权
    Process for the preparation of cyclopropylacetylene 有权
    环丙基乙炔的制备方法

    公开(公告)号：US06288297B1

    公开(公告)日：2001-09-11

    申请号：US09410481

    申请日：1999-09-30

    申请人： Zhe Wang ,  Jianguo Yin ,  Joseph M. Fortunak ,  Silvio Campagna

    发明人： Zhe Wang ,  Jianguo Yin ,  Joseph M. Fortunak ,  Silvio Campagna

    IPC分类号： C07C1207

    CPC分类号： C07C1/20 ,  C07C13/04 ,  C07C2601/02

    摘要： The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.

    摘要翻译： 本发明一般涉及用于合成环己基乙炔的新方法，其是不对称合成（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1 苯并恶嗪-2-酮; 一种有用的人类免疫缺陷病毒（HIV）逆转录酶抑制剂。 在此过程中，例如将环丙烷甲醛烷基化形成1,1,1-三氯-2-环丙基 - 乙醇; 其又被羟基保护形成1,1,1-三氯-2-环丙基乙基苯磺酸盐; 其又进行消除以形成环丙基乙炔。 这种改进提供了廉价的，容易获得的起始原料转化成环丙基乙炔的高转化率，高的总收率并且可以在工业规模上进行。

    Process for the preparation of macrocyclic metalloprotease inhibitors
    4.
    发明授权
    Process for the preparation of macrocyclic metalloprotease inhibitors 失效
    制备大环金属蛋白酶抑制剂的方法

    公开(公告)号：US06562963B2

    公开(公告)日：2003-05-13

    申请号：US09919564

    申请日：2001-07-31

    申请人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    发明人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    IPC分类号： C07C23101

    CPC分类号： C07C69/007 ,  C07C43/315 ,  C07C59/58 ,  C07C235/28 ,  C07D267/00 ,  C07D273/02

    摘要： The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

    摘要翻译： 本发明涉及制备式（Xa）化合物或其药学上可接受的盐形式的方法，其中：R 1选自：被0-5个R 1a取代的C 1-5烷基， - （O）R-C3-10环烷基取代有0-5个R 1a和 - （CH 2）r - 被0-5个R 1a取代的芳基。式（Ⅹa）化合物是含有抗琥珀酸残基的大环分子，其抑制金属蛋白酶如 聚集蛋白聚糖酶，以及肿瘤坏死因子（TNF）的产生。 抗琥珀酸盐由爱立信选择性的甲硅烷基乙烯酮缩醛的爱尔兰克莱森重排形成。