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1. 发明申请

WO2006122117A3 ORGANOMETAL BENZENEPHOSPHONATE COUPLING AGENTS 审中-公开
标题翻译：有机合成苯醌磷酸酯偶联剂
公开(公告)号：WO2006122117A3
公开(公告)日：2007-01-18
申请号：PCT/US2006017914
申请日：2006-05-09
申请人： MICROBIA INC , ZIMMER DANIEL P , TALLEY JOHN J
发明人： ZIMMER DANIEL P , TALLEY JOHN J
IPC分类号： A61K31/70
CPC分类号： C07F9/3834 , C07F9/4021 , C07F9/568
摘要： The invention relates to chemical genera of organometal benzenephosphonates useful in cross-coupling organic synthesis, having general formula (I): where R is selected from boron, zinc, tin and silicon residues.
摘要翻译：本发明涉及可用于交叉偶联有机合成的有机金属苯膦酸酯的化学属性，具有通式（I）：其中R选自硼，锌，锡和硅残基。

2. 发明申请

WO2006122117A2 ORGANOMETAL BENZENEPHOSPHONATE COUPLING AGENTS 审中-公开
标题翻译：有机合成苯醌磷酸酯偶联剂
公开(公告)号：WO2006122117A2
公开(公告)日：2006-11-16
申请号：PCT/US2006/017914
申请日：2006-05-09
申请人： MICROBIA, INC. , ZIMMER, Daniel, P. , TALLEY, John, J.
发明人： ZIMMER, Daniel, P. , TALLEY, John, J.
IPC分类号： C07D205/08
CPC分类号： C07F9/3834 , C07F9/4021 , C07F9/568
摘要： The invention relates to chemical genera of organometal benzenephosphonates useful in cross-coupling organic synthesis, having general formula (I): where R is selected from boron, zinc, tin and silicon residues.
摘要翻译：本发明涉及可用于交叉偶联有机合成的有机金属苯膦酸化合物，具有通式（I）：其中R选自硼，锌，锡和硅残基。

3. 发明申请

WO1991010646A1 1-AZETIDYL AND 1-HEXAMETHYLENIMINE ALKYL OR ARYL BISPHOSPHONIC ACIDS AND THEIR USE AS PHARMACOLOGICAL AGENTS 审中-公开
标题翻译： 1-季戊四醇和1-十六烷基亚胺碱或亚苄基双膦酸及其作为药物代谢物的用途
公开(公告)号：WO1991010646A1
公开(公告)日：1991-07-25
申请号：PCT/US1991000055
申请日：1991-01-03
申请人： RORER INTERNATIONAL (HOLDINGS), INC. , YOUSSEFYEH, Raymond, D. , CHENEY, Daniel, L. , BURNS, Christopher, J.
发明人： RORER INTERNATIONAL (HOLDINGS), INC.
IPC分类号： C07D205/04
CPC分类号： C07F9/6561 , C07F9/5532 , C07F9/568
摘要： This invention relates to compounds having: (A) a bisphosphonic acid endgroup; (B) an azetidine- or hexamethylenimine-derived azacyclic endgroup; and (C) an alkyl and/or aryl group linking the bisphosphonic acid and azacyclic groups through the nitrogen atom of the azacyclic group. These compounds are useful as agents for regulating the metabolism of polyvalent ions, particularly calcium. This invention relates also to pharmaceutical compositions including said compounds and to methods of treating conditions for which said metabolism is involved by using said compounds.
摘要翻译：本发明涉及具有：（A）双膦酸端基的化合物; （B）氮杂环丁烷或六亚甲基亚胺衍生的氮杂环端基; 和（C）通过氮杂环基的氮原子连接双膦酸和氮杂环基的烷基和/或芳基。这些化合物可用作调节多价离子，特别是钙的代谢的试剂。本发明还涉及包含所述化合物的药物组合物以及通过使用所述化合物治疗所述新陈代谢所涉及的病症的方法。

4. 发明申请

WO2008097819A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2008097819A2
公开(公告)日：2008-08-14
申请号：PCT/US2008/052735
申请日：2008-02-01
申请人： SMITHKLINE BEECHAM CORPORATION , COFFIN, Aaron , EVINDAR, Ghotas , YAO, Gang
发明人： COFFIN, Aaron , EVINDAR, Ghotas , YAO, Gang
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , C07D207/12 , C07D207/16 , C07F9/5532 , C07F9/568 , C07F9/5722 , C07F9/592 , C07F9/65583
摘要： The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.
摘要翻译：本发明提供了式I化合物，其制备以及它们作为药物活性免疫抑制剂用于治疗自身免疫病症，器官移植排斥，与激活的免疫系统相关的病症以及其他病症的用途受淋巴细胞减少或S1P受体调节。

5. 发明申请

WO2008057948A3 PROCESSES FOR PRODUCTION OF DIPHENYLYLAZETIDIN-2-ONES AND RELATED COMPOUNDS 审中-公开
标题翻译：生产二苯基吖丁啶-2-酮及相关化合物的方法
公开(公告)号：WO2008057948A3
公开(公告)日：2008-08-07
申请号：PCT/US2007083347
申请日：2007-11-01
申请人： IRONWOOD PHARMACEUTICALS INC , TALLEY JOHN J , MARTINEZ EDUARDO J
发明人： TALLEY JOHN J , MARTINEZ EDUARDO J
IPC分类号： C07H7/04 , C07D205/08
CPC分类号： C07D205/08 , C07C47/57 , C07C47/575 , C07C249/02 , C07D263/24 , C07D263/26 , C07F9/4021 , C07F9/568 , C07F9/5722 , C07F9/65062 , C07F9/653 , C07F9/6536 , C07F9/6539 , C07H7/04 , C07C251/24
摘要： Processes for preparing a 4-biphenylylazetidinone of formula are described. The processes generally proceed by either cyclizing a biphenylyl-ßaminoacyl compound or by arylating a 1-unsubstituted 4-biphenylylazetidinone with an R 1 -substituted phenyl arylating agent. Many of the processes may also be applied to the synthesis of 1,4-diphenylazetidinone deriviatives.
摘要翻译：描述了制备式的4-联苯基氮杂环丁酮的方法。该方法通常通过将联苯基 - β-氨基酰基化合物环化或通过用R 1 - 取代的苯基芳基化试剂将1-未取代的4-联苯基氮杂环丁烷酮芳基化来进行。许多方法也可用于合成1,4-二苯基氮杂环丁酮衍生物。

6. 发明申请

WO1993019070A1 CARBAPENEM DERIVATIVES AS ANTIBIOTICS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：卡巴因衍生物作为抗生素及其中间体
公开(公告)号：WO1993019070A1
公开(公告)日：1993-09-30
申请号：PCT/GB1993000603
申请日：1993-03-24
申请人： ZENECA LIMITED , ZENECA Pharma S.A. , JUNG, Frédéric, Henri
发明人： ZENECA LIMITED , ZENECA Pharma S.A.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , C07D409/12 , C07D409/14 , C07F9/568
摘要： The present invention relates to carbapenems and provides a compound of formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; and the thienyl ring is optionally further substituted by one or two substituents selected from halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, trifluoromethyl, C1-4alkoxycarbonyl, amino, C1-4alkylamino, di-C1-4alkylamino, sulfonic acid, C1-4alkylS(O)n- (wherein n is 0-2), C1-4alkanoylamino, C1-4alkanoyl(N &cir& _-C1-4alkyl)amino, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl and N &cir& _-C1-4alkanesulfonamido; or by a tetramethylene group attached to adjacent carbon atoms on the thienyl ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及碳青霉烯并提供式（I）化合物，其中：R 1是1-羟乙基，1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3是氢或C 1-4烷基; 噻吩基环任选被一个或两个选自卤素，氰基，C 1-4烷基，硝基，羟基，羧基，C 1-4烷氧基，三氟甲基，C 1-4烷氧基羰基，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，磺酸，C 1-4烷基S（O）n-（其中n为0-2），C 1-4烷酰基氨基，C 1-4烷酰基（N 1 -C 1-4烷基）氨基，氨基甲酰基，C 1-4烷基氨基甲酰基，和N和C 1-4烷基磺酰胺基; 或通过连接在噻吩环上相邻碳原子上的四亚甲基; 或其药学上可接受的盐或体内可水解的酯。还描述了其制备方法，其制备中的中间体，它们作为治疗剂的用途和含有它们的药物组合物。

7. 发明申请

WO1992017481A1 ANTIBIOTIC CARBAPENEM DERIVATIVES 审中-公开
标题翻译：抗生素CARBAPENEM衍生物
公开(公告)号：WO1992017481A1
公开(公告)日：1992-10-15
申请号：PCT/GB1992000588
申请日：1992-04-02
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA , BETTS, Michael, John , SWAIN, Michael, Lingard
发明人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , C07C229/56 , C07C229/62 , C07C229/64 , C07C233/54 , C07D207/16 , C07D403/12 , C07F9/568
摘要： A carbapenem compound of the formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; R is hydroxy or carboxy; and the phenyl ring is optionally further substituted by one or two substitutents selected from halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, trifluoromethyl, C1-4alkoxycarbonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl, amino, C1-4alkylamino, di-C1-4alkylamino, sulphonic acid, C1-4alkylS(O)n- (wherein n is 0-2), N-C1-4alkanesulphonamido, C1-4alkanoylamino and C1-4alkanoyl(N-C1-4alkyl)amino: provided that the phenyl ring is substituted by at least one carboxy; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.

8. 发明申请

WO1982001872A1 AZETIDINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： AZETIDINE衍生物及其制备方法
公开(公告)号：WO1982001872A1
公开(公告)日：1982-06-10
申请号：PCT/JP1980000296
申请日：1980-12-05
申请人： TAKEDA CHEM IND LTD
发明人： TAKEDA CHEM IND LTD , MATSUO TAISUKE , NOGUCHI NORIYOSHI , MASUYA HIROTOMO , OCHIAI MICHIHIKO
IPC分类号： C07D205/08
CPC分类号： C07D205/085 , C07D205/095 , C07F7/0812 , C07F7/10 , C07F9/568
摘要： 1-Sulfo-2-oxoazetidine derivatives represented by the following general formula (I): (FORMULA) [wherein R u represents an optionally acylated or protected amino group, X represents a hydrogen atom or a methoxy group, and R u represents an azido group or a group represented by (FORMULA) (wherein R u represents an organic residue, and n represents 0, 1 or 2)], and a process for their preparation as shown below: (FORMULA) [wherein R u represents an acylated or protected amino group, R u represents an acylated amino group, and R u and R u are as defined above].
摘要翻译：由以下通式（I）表示的1-磺基-2-氧代氮杂环丁烷衍生物：（式）其中R u表示任选酰化或保护的氨基，X表示氢原子或甲氧基， u表示叠氮基或由（式）表示的基团（其中R u表示有机残基，n表示0,1或2）]及其制备方法如下所示：（公式）[其中R u表示酰化或保护的氨基，R u表示酰化氨基，R u和R u如上所定义]。

9. 发明申请

WO2008097819A3 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2008097819A3
公开(公告)日：2008-11-13
申请号：PCT/US2008052735
申请日：2008-02-01
申请人： SMITHKLINE BEECHAM CORP , COFFIN AARON , EVINDAR GHOTAS , YAO GANG
发明人： COFFIN AARON , EVINDAR GHOTAS , YAO GANG
IPC分类号： C07D207/12 , C07D207/16
CPC分类号： A61K31/403 , C07D207/12 , C07D207/16 , C07F9/5532 , C07F9/568 , C07F9/5722 , C07F9/592 , C07F9/65583
摘要： The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.
摘要翻译：本发明提供了式I化合物，其制备方法及其作为药物活性免疫抑制剂用于治疗自身免疫病症，器官移植排斥反应，与激活的免疫系统相关的病症以及由淋巴细胞减少症或S1P受体调节的其他病症的用途。

10. 发明申请

WO2006127893A2 PROCESSES FOR PRODUCTION OF 4-(BIPHENYLYL)AZETIDIN-2-ONE PHOSPHONIC ACIDS 审中-公开
标题翻译：生产4-（二苯基）亚甲基-2-酮磷酸的方法
公开(公告)号：WO2006127893A2
公开(公告)日：2006-11-30
申请号：PCT/US2006020226
申请日：2006-05-25
申请人： MICROBIA INC , ANTONELLI STEPHEN , BARDEN TIMOTHY C , LEE PETER , MARTINEZ EDUARDO , SCHAIRER WAYNE C , TALLEY JOHN J
发明人： ANTONELLI STEPHEN , BARDEN TIMOTHY C , LEE PETER , MARTINEZ EDUARDO , SCHAIRER WAYNE C , TALLEY JOHN J
IPC分类号： A61P3/06 , A61K31/397 , A61K31/662 , C07C251/16 , C07D205/08 , C07D263/26 , C07F5/02 , C07F9/568
CPC分类号： C07C251/24 , C07D205/08 , C07D263/26 , C07D309/30 , C07D309/38 , C07F7/1892 , C07F9/568 , C07F9/5683
摘要： The present invention relates to processes for the production of 4-(biphenylyl)azetidin-2-one phosphonic acid derivatives of formula.
摘要翻译：本发明涉及制备下式的4-（联苯基）吖丁啶-2-酮膦酸衍生物的方法。

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