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1. 发明授权

US06177565B1 Process for synthesizing piperazic acid 有权
标题翻译：哌嗪酸合成方法
公开(公告)号：US06177565B1
公开(公告)日：2001-01-23
申请号：US09235894
申请日：1999-01-22
申请人： Andrea L. C. Robidoux
发明人： Andrea L. C. Robidoux
IPC分类号： C07D23104
CPC分类号： C07D487/04
摘要： The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of either or both processes in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).
摘要翻译：本发明涉及一种合成哌嗪酸和类似的含环酸的方法。本发明还涉及同时进行N（2） - 酰化哌嗪酸或其酯并形成双环结构的方法。本发明还涉及在合成可用作产生半胱天冬酶抑制剂，特别是白细胞介素-1β转换酶抑制剂（“ICE”）的中间体的双环化合物的方法中的任一方法或两种方法的用途。

2. 发明授权

US06252072B1 Method for producing nitroguanidine derivatives 失效
标题翻译：制备硝基胍衍生物的方法
公开(公告)号：US06252072B1
公开(公告)日：2001-06-26
申请号：US09445608
申请日：1999-12-08
申请人： Peter Maienfisch , Hansjürg Widmer
发明人： Peter Maienfisch , Hansjürg Widmer
IPC分类号： C07D23104
CPC分类号： C07D213/89 , C07D213/61 , C07D277/28 , C07D307/14 , C07D403/06
摘要： A process for the preparation of compounds of formula is described, wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl or a radical —CH2B; A is an unsubstituted or mono- to penta-substituted, aromatic or non-aromatic, monocyclic to bicyclic heterocyclic radical; and B is phenyl, 3-pyridyl or thiazolyl, which are optionally substituted by one to rhee substituents; by means of the hydrolysis of a compound of formula wherein R1, R2 and A have the same significances as given for formula (I), and R3 signifies unsubstituted or substituted C1-C10-alkyl, C3-C6-cycloalkyl, phenyl or benzyl; whereby the reaction is carried out at a pH value of between 7 and 14, as well as starting materials for carrying out the process. The compounds of formula (I) are suitable as intermediates in the preparation of pesticidal compositions.
摘要翻译：一种制备式中化合物的方法，其中R 1是氢或C 1 -C 4 - 烷基; R 2是氢，C 1 -C 6烷基，C 3 -C 6环烷基或基团-CH 2 B; A是未取代的或单 - 五取代的，芳族的或非芳香的单环到双环杂环基; 和B是苯基，3-吡啶基或噻唑基，它们任选地被一个取代基取代;通过水解式I的化合物，R 2和A具有与式（I）给出的相同的含义，并且R 3表示未取代或取代的C 1 -C 10 - 烷基，C 3 -C 6 - 环烷基，苯基或苄基; 由此反应在7-14之间的pH值下进行，以及用于进行该方法的起始原料。式（I）化合物适合作为制备杀虫剂组合物的中间体。

3. 依法登记的发明

USH1942H1 Herbicidal 3-(pyrazolylphenyl)propanoic acids and derivatives 失效
公开(公告)号：USH1942H1
公开(公告)日：2001-02-06
申请号：US09144773
申请日：1998-09-01
申请人： George Theodoridis , Scott D. Crawford , Lester L. Maravetz
发明人： George Theodoridis , Scott D. Crawford , Lester L. Maravetz
IPC分类号： C07D23104
摘要： Novel herbicidal compounds, compositions containing them, and methods for their preparation and use in controlling weeds are disclosed. The novel herbicidal compounds are 3-(pyrazolylphenyl)propanoic acids and derivatives having the formula: wherein X is H or halogen; Y is halogen, trihaloalkyl or cyano; Z and R are halogen; R1 is carboxyl or agriculturally acceptable salt thereof, cyano, alkoxycarbonyl, alkylthiocarbonyl, alkoxyalkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, or alkylsulfonylaminocarbonyl; and R2 is hydrogen or lower alkyl.

4. 发明授权

US06809206B2 Method for acylating cyclic compounds 失效
标题翻译：酰化环状化合物的方法
公开(公告)号：US06809206B2
公开(公告)日：2004-10-26
申请号：US10396047
申请日：2003-03-24
申请人： Paul Walter Wojtkowski
发明人： Paul Walter Wojtkowski
IPC分类号： C07D23104
CPC分类号： C07D495/10 , C07C45/455 , C07C45/64 , C07C46/00 , C07C49/403 , C07C49/67 , C07C49/697 , C07C49/713 , C07C49/747 , C07C49/753 , C07C49/792 , C07C49/813 , C07C49/835 , C07C50/28 , C07C315/04 , C07C317/24
摘要： The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.
摘要翻译：本发明的方法通过在氰化物或氟化物催化剂存在下使苯基酯作为酰化剂与环状化合物接触来制备酰化的环状化合物。

5. 发明授权

US06455703B2 1,3,6,-Trihydro-6-aza-3-oxapentalen-2-one derivatives for the treatment of neoplasia 失效
标题翻译： 1,3,6 - 三氢-6-氮杂-3-氧杂蒽环-2-酮衍生物用于治疗肿瘤
公开(公告)号：US06455703B2
公开(公告)日：2002-09-24
申请号：US09731570
申请日：2000-12-06
申请人： Gerhard Sperl , Rifat Pamukcu
发明人： Gerhard Sperl , Rifat Pamukcu
IPC分类号： C07D23104
CPC分类号： C07D491/04 , A61K31/407
摘要： 1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives which have the following formula: wherein R1, R2, R3, R4, R5, Y, X, m, and n are as defined in the specification.
摘要翻译：具有下式的1,3,6-三氢-6-氮杂-3-氧杂心嘌呤-2-酮衍生物：其中R1，R2，R3，R4，R5，Y，X，m和n如规范。

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