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1. 发明申请

WO2011056744A1 IRE-1 α INHIBITORS 审中-公开
标题翻译： IRE-1一个抑制剂
公开(公告)号：WO2011056744A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/054940
申请日：2010-11-01
申请人： MANNKIND CORPORATION , ZENG, Qingping , WADE, Warren S. , PATTERSON, John Bruce
发明人： ZENG, Qingping , WADE, Warren S. , PATTERSON, John Bruce
IPC分类号： A61K31/185 , A61K31/27
CPC分类号： C07D487/08 , C07C59/74 , C07C65/30 , C07C69/738 , C07C235/78 , C07C235/84 , C07D207/08 , C07D207/14 , C07D207/16 , C07D211/26 , C07D211/58 , C07D211/62 , C07D211/66 , C07D211/98 , C07D213/36 , C07D213/38 , C07D213/74 , C07D213/81 , C07D213/82 , C07D239/26 , C07D239/38 , C07D249/06 , C07D263/34 , C07D277/12 , C07D277/18 , C07D277/42 , C07D277/56 , C07D295/108 , C07D295/112 , C07D295/185 , C07D295/192 , C07D295/26 , C07D295/32 , C07D307/68 , C07D333/38 , C07D333/40 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The invention provides compounds which directly inhibit IRE-1α activity in vitro , prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译：本发明提供了在体外直接抑制IRE-1a活性的化合物，其前药和药学上可接受的盐。这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病，并可用作单一药剂或联合疗法。

2. 发明申请

WO00005197A1 PHOTOCLEAVABLE AND ACID CLEAVABLE LINKERS FOR COMBINATORIAL CHEMISTRY 审中-公开
标题翻译：用于组合化学的光电和酸性可清洗的连接器
公开(公告)号：WO00005197A1
公开(公告)日：2000-02-03
申请号：PCT/US1999/016798
申请日：1999-07-22
IPC分类号： C07B61/00 , C07C59/74 , C07C205/37 , C07C205/44 , C07C235/06 , C08F8/28 , C08F8/30 , C07C59/325 , C07C69/712
CPC分类号： C40B80/00 , C07B2200/11 , C07C59/74 , C07C205/37 , C07C205/44 , C07C235/06
摘要： A substrate for solid phase synthesis comprising a solid phase-linker combination of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediate useful therein. Among the novel intermediates are compounds of formula (II) wherein R is -NO2 or -CHO; R is -OCH3, -CHO or -H; R is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n = 1 or 3-12. A substrate of solid phase synthesis of formula (III) is also disclosed.
摘要翻译：公开了用于固相合成的底物，其包含式（I）的固相 - 连接体组合。还公开了制备其中有用的基材和化学中间体的方法。其中新的中间体是式（II）的化合物，其中R 1是-NO 2或-CHO; R 2是-OCH 3，-CHO或-H; R 3选自羟基，具有多个氨基的固体支持物的残基和酯的残基，n = 1或3-12。还公开了式（III）的固相合成的底物。

3. 发明申请

WO1997036852A1 NOVEL BENZALDEHYDE DERIVATIVES FROM HERICEUM ERINACEUS 审中-公开
标题翻译：新的苯甲醛衍生物FROM HERICEUM刺猬
公开(公告)号：WO1997036852A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001504
申请日：1997-03-25
申请人： HOECHST AKTIENGESELLSCHAFT , STUMP, Heike , STAHL, Wilhelm , WINK, Joachim , WINKLER, Irvin , KOGLER, Herbert , BACKHAUS, Jürgen
发明人： HOECHST AKTIENGESELLSCHAFT
IPC分类号： C07C59/90
CPC分类号： C07C59/74 , C12P7/42
摘要： The present invention relates to a compound of formula (I) R to R are hydrogen or methyl, where two R to R on adjacent carbon atoms together with a C-C single bond may stand for a C-C double bond, provided that, in the carbon chain substituted by R to R , only one of the substituents R to R is methyl and only an adjacent pair of said substituents contribute to a C-C double bond, a process for its production and its use as a medicament, especially for treating diseases produced by an HIV infection.
摘要翻译：本发明涉及式（I）的化合物，其中R <1>至R <10>为氢或甲基，其中两个相邻碳原子上利用Dende，R <1>至R <10>与CC-单键用于一起一个C-C双键的可自由基，条件是在其中R <1>至R <10>在每一种情况下的碳链仅取代基的一个R <1>至R <10>取代是甲基并且只有一对相邻的这些取代基的有助于一个CC-双键，它们的制备方法和它们作为药物的用途的方法，尤其是用于由HIV感染引起的疾病的治疗。

4. 发明申请

WO2018090717A1 ATG类似物及其制备方法和应用审中-公开
公开(公告)号：WO2018090717A1
公开(公告)日：2018-05-24
申请号：PCT/CN2017/102936
申请日：2017-09-22
申请人：上海中医药大学附属龙华医院
发明人：钟逸斐 , 何慈江 , 戴思巴斯卡 , 刘睿捷
IPC分类号： C07F5/02 , C07C59/64 , C07C59/74 , C07C43/23 , C07C49/255 , C07D307/33 , A61K31/69 , A61P43/00
CPC分类号： A61K31/69 , A61P43/00 , C07C43/23 , C07C49/255 , C07C59/64 , C07C59/74 , C07D307/33 , C07F5/02
摘要：本发明提供ATG类似物及其制备方法和应用，ATG类似物的具体结构如下列三个通式所示: 式(I)，式(II)，式(III) 其中，X/Y/Z可以分别选自C、N、S、O, R 1， R 2， R 3， R 4， R 5 各自分别选自: H，CH 3 基团，脂肪族或者芳香族碳氢化合物基团，硝基，磷酸基，硫化物基团，砜类基团，腈类基团，杂环基，硼酸酯或硼酸基团，酯类基团，胺类基团。本发明所提供的ATG类似物具有更好的水溶性和防止在一级代谢中被分解的效果。

5. 发明申请

WO2008127646A8 TRANSAMINASE-BASED PROCESSES FOR PREPARATION OF PREGABALIN 审中-公开
标题翻译：用于制备PREGABALIN的基于分散蛋白酶的方法
公开(公告)号：WO2008127646A8
公开(公告)日：2009-02-26
申请号：PCT/US2008004699
申请日：2008-04-10
申请人： BIOVERDANT INC , NOTZ WOLFGANG REINHARD LUDWIG , SCOTT ROBERT WILLIAM , ZHAO LISHAN , TAO JUNHUA
发明人： NOTZ WOLFGANG REINHARD LUDWIG , SCOTT ROBERT WILLIAM , ZHAO LISHAN , TAO JUNHUA
CPC分类号： C07C229/08 , C07C45/41 , C07C51/09 , C07C51/377 , C07C67/343 , C07C69/716 , C07C227/08 , C07D307/33 , C12P13/001 , C07C47/02 , C07C59/225 , C07C59/74
摘要： Provided herein are compounds and processes to prepare intermediates and precursors of pregabalin and related compositions, and processes for the preparation of pregabalin.
摘要翻译：本文提供了制备普瑞巴林及相关组合物的中间体和前体的化合物和方法，以及制备普瑞巴林的方法。

6. 发明申请

WO03087824A2 ORGANIC MOLECULES 审中-公开
标题翻译：有机分子
公开(公告)号：WO03087824A2
公开(公告)日：2003-10-23
申请号：PCT/GB0301505
申请日：2003-04-07
申请人： AMURA THERAPEUTICS LTD , FLINN NICHOLAS SEAN , QUIBELL MARTIN , TURNELL WILLIAM GORDON , RAMJEE MANOJ KUMAR
发明人： FLINN NICHOLAS SEAN , QUIBELL MARTIN , TURNELL WILLIAM GORDON , RAMJEE MANOJ KUMAR
IPC分类号： A61K47/48 , B01D67/00 , C07C59/74 , C07K7/06 , G01N33/543
CPC分类号： B01D67/0093 , A61K47/646 , A61K47/65 , C07C59/74 , C07K7/06
摘要： Compounds according to general formulae (Ia to Ie) wherein: X = O or S; Y is O, S or CH2, CHR, CRR, where R is C1-7 alkyl; Z is O or S; R1 is H or C1-7 alkyl; R2 is H or C1-7 alkyl; R4 is H or C1-7 alkyl at any vacant position on the aromatic ring; R3 is C1-7 alkyl-L1-R5-L2- R6-COOH, C3-10 cycloalkyl-L1-R5-L2- R6-COOH or Ar-C0-7 alkyl-L1-R5-L2- R6-COOH; each of L1 and L2 is absent or a suitable linker such as an amide CONH; or an ether -O-, or a thioether -S- or a sulphone -S02-; R5 is C1-7 alkyl, C3-1O cycloalkyl or Ar-C0-7 alkyl each of which is substituted with either NR8R9, where the nitrogen atom is capable of being protonated in solution to give N HR8R9; or a quaternary nitrogen atom N R8R9R10, such that R5 contains a positive charge; each of R8, R9 and R10 is independently C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl, or any two or more of R8, R9 and R10 together form an alicyclic or arylalicyclic ring system; R6 is C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl; and their salts, hydrates, solvates, complexes or prodrugs are of use as linkers for conjugating an epitope to a carrier protein.
摘要翻译：根据通式（Ia至Ie）的化合物，其中：X = O或S; Y是O，S或CH 2，CHR，CRR，其中R是C 1-7烷基; Z是O或S; R1是H或C1-7烷基; R2是H或C1-7烷基; R4是芳环上任何空位的H或C 1-7烷基; R3是C1-7烷基-L1-R5-L2-R6-COOH，C3-10环烷基-L1-R5-L2-R6-COOH或Ar-C10-烷基-L1-R5-L2-R6-COOH; L1和L2各自不存在，或者合适的接头如酰胺CONH; 或醚-O-，或硫醚-S-或砜-S02-; R5是C1-7烷基，C3-1O环烷基或任选被NR8R9取代的Ar-C0-7烷基，其中氮原子能够在溶液中被质子化，得到N + HR8R9; 或季氮原子N + R 8 R 9 R 10，使得R 5含有正电荷; R 8，R 9和R 10各自独立地为C 1-7烷基，C 3-10环烷基或Ar-C 0-7烷基，或R 8，R 9和R 10中的任何两个或更多个一起形成脂环族或芳基脂环族环系; R 6是C 1-7烷基，C 3-10环烷基或Ar-C 0-7烷基; 并且它们的盐，水合物，溶剂合物，复合物或前药可用作将表位与载体蛋白缀合的接头。

7. 发明申请

WO9817628A3 A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF AMIDES 审中-公开
标题翻译：一种用于制备AMIDES的固相技术
公开(公告)号：WO9817628A3
公开(公告)日：1998-09-03
申请号：PCT/GB9702914
申请日：1997-10-22
申请人： PEPTIDE THERAPEUTICS LTD , JOHNSON TONY , QUIBELL MARTIN
发明人： JOHNSON TONY , QUIBELL MARTIN
IPC分类号： C07D241/08 , C07B61/00 , C07C47/565 , C07C51/367 , C07C59/74 , C07C59/92 , C07C69/712 , C07C231/02 , C07C231/10 , C07C233/00 , C07K1/04 , C07K1/06 , C08F8/30 , C07C59/125 , C07C69/708 , C07K1/00
CPC分类号： C07C59/74 , C07C69/712 , C07C231/10 , C07K1/045 , C07K1/047
摘要： A method for the solid phase synthesis of compounds of formula (1), in which either or both of R1 or R2 are combinatorially variable by a process represented by scheme (4) and wherein: X is (a), (b), (c) or (d); Y is H or a side chain functional group protective moiety such as Fmoc; R21 is an intermediate form of R2 which is subsequently chemically transformed to give the desired R2; and n is between 2 and 12, preferably 4. The invention also provides compounds and combinatorial libraries of compounds of formula (1), as well as intermediate compounds for use in the method.

8. 发明申请

WO2011056744A4 IRE-1 a INHIBITORS 审中-公开
标题翻译： IRE-1 a抑制剂
公开(公告)号：WO2011056744A4
公开(公告)日：2011-07-14
申请号：PCT/US2010054940
申请日：2010-11-01
申请人： MANNKIND CORP , ZENG QINGPING , WADE WARREN S , PATTERSON JOHN BRUCE
发明人： ZENG QINGPING , WADE WARREN S , PATTERSON JOHN BRUCE
IPC分类号： A61K31/185 , A61K31/27
CPC分类号： C07D487/08 , C07C59/74 , C07C65/30 , C07C69/738 , C07C235/78 , C07C235/84 , C07D207/08 , C07D207/14 , C07D207/16 , C07D211/26 , C07D211/58 , C07D211/62 , C07D211/66 , C07D211/98 , C07D213/36 , C07D213/38 , C07D213/74 , C07D213/81 , C07D213/82 , C07D239/26 , C07D239/38 , C07D249/06 , C07D263/34 , C07D277/12 , C07D277/18 , C07D277/42 , C07D277/56 , C07D295/108 , C07D295/112 , C07D295/185 , C07D295/192 , C07D295/26 , C07D295/32 , C07D307/68 , C07D333/38 , C07D333/40 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The invention provides compounds which directly inhibit IRE-1a activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译：本发明提供了直接抑制体外IRE-1a活性的化合物，其前体药物和药学上可接受的盐。此类化合物和前药可用于治疗与未折叠的蛋白质应答有关的疾病，并可用作单一药剂或组合疗法。

9. 发明申请

WO2008127646A2 TRANSAMINASE-BASED PROCESSES FOR PREPARATION OF PREGABALIN 审中-公开
标题翻译：用于制备PREGABALIN的基于分散蛋白酶的方法
公开(公告)号：WO2008127646A2
公开(公告)日：2008-10-23
申请号：PCT/US2008004699
申请日：2008-04-10
申请人： BIOVERDANT INC , NOTZ WOLFGANT REINHARD LUDWIG , SCOTT ROBERT WILLIAM , ZHAO LISHAN , TAO JUNHUA
发明人： NOTZ WOLFGANT REINHARD LUDWIG , SCOTT ROBERT WILLIAM , ZHAO LISHAN , TAO JUNHUA
CPC分类号： C07C229/08 , C07C45/41 , C07C51/09 , C07C51/377 , C07C67/343 , C07C69/716 , C07C227/08 , C07D307/33 , C12P13/001 , C07C47/02 , C07C59/225 , C07C59/74
摘要： Provided herein are compounds and processes to prepare intermediates and precursors of pregabalin and related compositions, and processes for the preparation of pregabalin.
摘要翻译：本文提供了制备普瑞巴林及相关组合物的中间体和前体的化合物和方法，以及制备普瑞巴林的方法。

10. 发明申请

WO2006076370B1 SUBSTITUTED CYCLOPENTANES OR CYCLOPENTANONES FOR THE TREATMENT OF OCULAR HYPERTENSIVE CONDITIONS 审中-公开
标题翻译：替代性CYCLOPENTANES或CYCLOPENTANONES治疗OCULAR HYPERTENSIVE条件
公开(公告)号：WO2006076370B1
公开(公告)日：2007-02-22
申请号：PCT/US2006000831
申请日：2006-01-10
申请人： ALLERGAN INC , OLD DAVID W , GAC TODD S , NGO VINH X
发明人： OLD DAVID W , GAC TODD S , NGO VINH X
IPC分类号： C07C59/68 , A61K31/192 , A61K31/222 , A61P27/06 , C07C59/90 , C07C69/02 , C07C69/52
CPC分类号： C07C405/00 , A61K31/192 , A61K31/216 , A61K31/222 , C07C59/72 , C07C59/74 , C07C59/90 , C07C69/736 , C07C69/738 , C07C2601/08
摘要： The invention relates to the use of substituted cyclopentanes or cyclopentanones as ocular hypotensives. New Compounds are also provided.
摘要翻译：本发明涉及使用取代的环戊烷或环戊酮作为眼睛低血压剂。还提供新化合物。

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