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1. 发明申请

WO2016075062A1 2-AMINO-3,5-DIFLUORO-3,6-DIMETHYL-6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS FOR TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译： 2-氨基-3,5-二氟-3,6-二甲基-6-苯基-3,4,5,6-四氢吡啶作为BACE1抑制剂治疗阿尔茨海默病
公开(公告)号：WO2016075062A1
公开(公告)日：2016-05-19
申请号：PCT/EP2015/076014
申请日：2015-11-09
申请人： H. LUNDBECK A/S
发明人： JUHL, Karsten , TAGMOSE, Lena , MARIGO, Mauro
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , C07D211/72 , A61K31/444 , A61K31/497 , A61P25/28
CPC分类号： C07D211/72 , C07B59/002 , C07B2200/05 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention is directed to compounds according to Formula (I) which compounds are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for 5 which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中化合物是BACE1酶的抑制剂。本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗Aβ沉积物减少如Aβ阿尔茨海默氏病的病症的用途。

2. 发明申请

WO2010065512A2 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
标题翻译：治疗增殖性疾病的化合物
公开(公告)号：WO2010065512A2
公开(公告)日：2010-06-10
申请号：PCT/US2009/066211
申请日：2009-12-01
申请人： SYNTA PHARMACEUTICALS CORP. , JIANG, Jun , KOWALCZYK-PRZEWLOKA, Teresa , SCHWEIZER, Stefan M. , XIA, Zhi-Qiang , CHEN, Shoujun , BORELLA, Christopher , SUN, Lijun
发明人： JIANG, Jun , KOWALCZYK-PRZEWLOKA, Teresa , SCHWEIZER, Stefan M. , XIA, Zhi-Qiang , CHEN, Shoujun , BORELLA, Christopher , SUN, Lijun
IPC分类号： C07C327/56 , C07D213/86 , C07D263/34 , C07D277/56 , C07D295/16 , C07D317/62 , A61K31/175 , A61K31/36 , A61K31/40 , A61K31/421 , A61K31/426 , A61K31/4402 , A61P35/00
CPC分类号： C07D295/195 , C07C327/56 , C07C333/12 , C07C335/40 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/04 , C07D211/72 , C07D213/86 , C07D213/87 , C07D241/24 , C07D277/56 , C07D295/155 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/68
摘要： The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
摘要翻译：本发明涉及由结构式（I）表示的化合物，或其药学上可接受的盐或过渡金属螯合物，其配位体或络合物或去质子化的过渡金属螯合物，配位体或络合物化合物的形式。还包括这些化合物的药物组合物和使用方法。

3. 发明申请

WO2010026989A1 オルト置換ハロアルキルスルホンアニリド誘導体及び除草剤审中-公开
标题翻译： ORTHO取代的HALOALKYLSULFONANILIDE衍生和除草剂
公开(公告)号：WO2010026989A1
公开(公告)日：2010-03-11
申请号：PCT/JP2009/065343
申请日：2009-09-02
申请人：日産化学工業株式会社 , 工藤隆生 , 谷間大輔 , 舛沢禎英 , 矢野哲彦
发明人：工藤　隆生 , 谷間　大輔 , 舛沢　禎英 , 矢野　哲彦
IPC分类号： C07D205/08 , A01N43/36 , A01N43/40 , A01N43/44 , A01P13/02 , C07D207/27 , C07D211/72 , C07D211/76 , C07D213/64 , C07D221/20 , C07D223/10 , C07D239/06 , C07D239/10 , C07D243/04 , C07D491/044
CPC分类号： C07D211/76 , A01N43/36 , A01N43/40 , A01N43/44 , A01N43/46 , A01N43/50 , A01N43/54 , A01N43/62 , A01N47/04 , A01N47/24 , C07D211/72 , C07D221/20 , C07D221/22 , C07D223/10 , C07D223/32 , C07D239/06 , C07D239/10 , C07D239/36 , C07D491/044
摘要：　新規除草剤を提供すること　一般式（１）：〔〔式中、Ａは－Ｃ（Ｒ７）（Ｒ８）－又は－Ｎ（Ｒ９）－を表し、　Ｗは酸素原子又は硫黄原子を表し、ｎは１乃至４の整数を表し、Ｒ１はハロＣ１－Ｃ６アルキルを表し、Ｒ 2 は水素原子、Ｃ 1- Ｃ 6 アルキル等を表し、Ｒ 3 及びＲ 4 はそれぞれ独立に、水素原子、Ｃ 1- Ｃ 6 アルキル等を表し、Ｒ５、Ｒ６、Ｒ７及びＲ８はそれぞれ独立に、水素原子、ハロゲン、Ｃ 1- Ｃ 6 アルキル、等を表し、Ｒ９は水素原子、Ｃ１－Ｃ６アルキル等を表し、Ｘは、ハロゲン、Ｃ 1- Ｃ 6 アルキル等を表す。〕で表されるハロアルキルスルホンアニリド誘導体又は農薬として許容されるその塩類。
摘要翻译：公开了一种新型除草剂。具体公开的是由通式（1）表示的卤代烷基磺酰苯胺衍生物[其中A表示-C（R7）（R8） - 或-N（R9） - ; W表示氧原子或硫原子; n表示1〜4的整数， R1表示卤代-C1-C6烷基; R2表示氢原子，C1-C6烷基等; R3和R4独立地表示氢原子，C1-C6烷基等; R5，R6，R7和R8独立地表示氢原子，卤素，C1-C6烷基等; R9表示氢原子，C1-C6烷基等; X表示卤素，C 1 -C 6烷基等]或其农业上可接受的盐。

4. 发明申请

WO2008008398A2 OXIME COMPOUNDS AND THE USE THEREOF 审中-公开
标题翻译： OXIME化合物及其用途
公开(公告)号：WO2008008398A2
公开(公告)日：2008-01-17
申请号：PCT/US2007015827
申请日：2007-07-12
申请人： SHIONOGI & CO , EURO CELTIQUE SA , MATSUMURA AKIRA , MIKAMIYAMA HIDENORI , TSUNO NAOKI , KYLE DONALD J , SHAO BIN , YAO JIANGCHAO
发明人： MATSUMURA AKIRA , MIKAMIYAMA HIDENORI , TSUNO NAOKI , KYLE DONALD J , SHAO BIN , YAO JIANGCHAO
IPC分类号： A61K31/4468
CPC分类号： C07D211/72 , C07D211/96 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO 2 , CR 3 R 4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R 3 and R 4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is O, 1 or 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及式（I）的肟化合物及其药学上可接受的盐，前药或溶剂合物，其中X为氢，任选取代的芳基，任选取代的杂芳基等; Y是CO，SO 2，CR 3，R 4等; Z是任选取代的低级烷基，任选取代的芳基等; W是任选取代的低级亚烷基或任选取代的低级亚烯基，R 3和R 4各自独立地为氢，低级烷基等; p是0,1或2，q是0,1或2.本发明还涉及使用式I化合物来治疗，预防或改善对钙通道阻断有反应的病症，特别是N型钙通道。本发明的化合物特别可用于治疗疼痛。

5. 发明申请

WO2006057961A1 3-[2-(3-ACYLAMINO-2-OXO-2H-PYRIDIN-1-YL)-ACETYLAMINO]-4-OXO-PENTANOIC ACID DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS 审中-公开
标题翻译： 3- [2-（3-氨基亚氨基-2-氧代-2H-吡啶-1-基） - 乙酰氨基] -4-氧代戊酸衍生物及其作为CASPASE抑制剂的用途
公开(公告)号：WO2006057961A1
公开(公告)日：2006-06-01
申请号：PCT/US2005/042139
申请日：2005-11-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
发明人： CHARRIER, Jean-Damien , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
IPC分类号： C07D213/75 , A61K31/4412 , A61K31/4436 , A61K31/4439 , C07D401/06 , C07D409/06
CPC分类号： C07D213/75 , C07D211/72 , C07D401/02 , C07D401/06 , C07D409/06
摘要： The present invention provides a compound of formula (I): wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
摘要翻译：本发明提供式（I）化合物：其中R 1，R 2，R 3，R 3， > 4 ，＆lt; SUP＆gt;和R＆lt; 5＆gt;如本文所定义。本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及制备本发明化合物的方法。

6. 发明申请

WO0220526A3 CYCLIC AND ACYCLIC AMIDINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM FOR USE AS PROGESTERONE RECEPTOR BINDING AGENTS 审中-公开
标题翻译：包含它们作为孕激素受体结合剂的循环和ACYCLIC和药物组合物
公开(公告)号：WO0220526A3
公开(公告)日：2002-05-30
申请号：PCT/US0127007
申请日：2001-08-30
申请人： BAYER AG , BULLOCK WILLIAM H , KLUENDER HAROLD C E , COLLIBEE WILLIAM L , DALLY ROBERT , RODRIGUEZ MARTHA E , WANG MING
发明人： BULLOCK WILLIAM H , KLUENDER HAROLD C E , COLLIBEE WILLIAM L , DALLY ROBERT , RODRIGUEZ MARTHA E , WANG MING
IPC分类号： C07D295/12 , A61K31/136 , A61K31/155 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/426 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/47 , A61K31/496 , A61K31/5375 , A61K31/55 , A61P5/24 , A61P5/42 , A61P15/00 , A61P15/02 , A61P15/04 , A61P15/06 , A61P15/08 , A61P15/12 , A61P19/08 , A61P19/10 , A61P35/00 , A61P43/00 , C07C257/14 , C07D207/22 , C07D209/52 , C07D209/54 , C07D211/14 , C07D211/72 , C07D215/38 , C07D221/20 , C07D221/22 , C07D223/12 , C07D223/14 , C07D223/32 , C07D225/02 , C07D235/26 , C07D265/30 , C07D277/04 , C07D295/125 , C07D453/06 , C07D487/08 , A61K31/435 , C07D295/13
CPC分类号： C07D295/125 , A61K31/136 , A61K31/395 , A61K31/40 , A61K31/438 , A61K31/445 , A61K31/47 , A61K31/5375 , A61K31/55 , C07C257/14 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/22 , C07D211/72 , C07D221/22 , C07D223/32 , C07D487/08
摘要： Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.
摘要翻译：公开了环状和非环状脒基，含有这种脒的药物组合物及其在治疗或预防孕酮受体介导的疾病或病症如骨质减少和骨质疏松症中的用途。

7. 发明申请

WO02020526A2 CYCLIC AND ACYCLIC AMIDINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM FOR USE AS PROGESTERONE RECEPTOR BINDING AGENTS 审中-公开
标题翻译：含有这些化合物作为孕酮受体结合剂的环状和非环状氨基酸和药物组合物
公开(公告)号：WO02020526A2
公开(公告)日：2002-03-14
申请号：PCT/US2001/027007
申请日：2001-08-30
IPC分类号： C07D295/12 , A61K31/136 , A61K31/155 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/426 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/47 , A61K31/496 , A61K31/5375 , A61K31/55 , A61P5/24 , A61P5/42 , A61P15/00 , A61P15/02 , A61P15/04 , A61P15/06 , A61P15/08 , A61P15/12 , A61P19/08 , A61P19/10 , A61P35/00 , A61P43/00 , C07C257/14 , C07D207/22 , C07D209/52 , C07D209/54 , C07D211/14 , C07D211/72 , C07D215/38 , C07D221/20 , C07D221/22 , C07D223/12 , C07D223/14 , C07D223/32 , C07D225/02 , C07D235/26 , C07D265/30 , C07D277/04 , C07D295/125 , C07D453/06 , C07D487/08 , A61K31/435 , C07D295/13
CPC分类号： C07D295/125 , A61K31/136 , A61K31/395 , A61K31/40 , A61K31/438 , A61K31/445 , A61K31/47 , A61K31/5375 , A61K31/55 , C07C257/14 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/22 , C07D211/72 , C07D221/22 , C07D223/32 , C07D487/08
摘要： Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.
摘要翻译：本发明涉及环状和无环脒，含有这些脒的药物组合物及其在治疗或预防黄体酮受体介导的疾病或病症如骨质减少和骨质疏松症中的用途。

8. 发明申请

WO99037615A1 METHOD FOR PRODUCING (-)CIS-3-HYDROXY-1-METHYL-4-(2,4,6-TRIMETHOXYPHENYL)-PIPERIDINE 审中-公开
标题翻译：用于制备（ - ）顺-3-羟基-1-甲基-4-（2，4,6-三甲氧基苯基） - 哌啶
公开(公告)号：WO99037615A1
公开(公告)日：1999-07-29
申请号：PCT/EP1998/008327
申请日：1998-12-18
IPC分类号： C07D211/42 , C07D211/72 , C07D211/74 , C07D405/04
CPC分类号： C07D405/04 , C07D211/42 , C07D211/72 , C07D211/74
摘要： Disclosed is a method for producing (-)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-piperidine-hydrobromide and reacted with 1,3,5-trimethoxybenzol to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring. The product thus prepared is catalytically hydrogenated into a racemic 3,4-cis-alcahol and subsequently, enantiomerically pure (-)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine is obtained by separation of racemic mixtures with chiral auxiliary reagents from racemic 3,4-cis alcohol.
摘要翻译：它是用于制备方法（ - ）顺-3-羟基-1-甲基-4-（2,4,6-三甲氧基苯基） - 哌啶描述，其特征在于1-甲基哌啶-4- 上转化成氢溴酸盐，然后用溴，得到3（R，S） - 溴-1-甲基-4-氧代 - 哌啶氢溴酸盐，并进一步与1,3,5-三甲氧基苯向3（R，S） - 溴 1-甲基-4-（2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶氢溴酸盐反应。通过在有机溶剂中最初3（R，S）搅拌反应溶液溴-1-甲基-4-（2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶氢溴酸盐，其为固体分离，并随后加入到与水的产物，并通过搅拌，3（R，S） - 羟基-1-甲基-4-（2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶进行反应。当时工作式产物催化氢化，得到外消旋3,4-顺醇，然后通过与手性辅助试剂外消旋体拆分由外消旋3,4-顺醇的对映体纯的（ - ）顺-3-羟基-1-甲基-4- （2,4,6-三甲氧基苯基）哌啶获得。

9. 发明申请

WO1998016499A1 OXIME DERIVATIVES, HYDRAZONE DERIVATIVES, AND USE THEREOF 审中-公开
标题翻译： OXIME衍生物，HYDRAZONE衍生物及其用途
公开(公告)号：WO1998016499A1
公开(公告)日：1998-04-23
申请号：PCT/JP1997003585
申请日：1997-10-07
申请人： SHIONOGI & CO., LTD. , MASUI, Moriyasu , TANIMOTO, Norihiko , NISHIDA, Kuniyoshi
发明人： SHIONOGI & CO., LTD.
IPC分类号： C07C251/36
CPC分类号： C07D213/30 , A01N37/50 , A01N41/06 , A01N41/10 , A01N43/40 , A01N43/46 , A01N43/80 , A01N47/16 , C07C251/36 , C07C251/48 , C07C251/52 , C07C251/54 , C07C251/74 , C07C259/06 , C07D207/12 , C07D211/42 , C07D211/46 , C07D211/58 , C07D211/72 , C07D243/08 , C07D261/02 , C07D295/185 , C07D295/26 , C07D333/16 , C07D401/12
摘要： Compounds having bactericidal activities and represented by general formula (I) and salts and hydrates thereof wherein R represents an optionally substituted aryl, an optionally substituted alkyl or the like; R represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R and R , which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R and R may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR (wherein R represents a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted alkanoyl, or an optionally substituted aroyl); Z represents an oxygen atom or a sulfur atom; and a wavy line ( SIMILAR ) represents the configuration of an E isomer, a Z isomer, or a mixture thereof.
摘要翻译：具有杀菌活性并由通式（I）表示的化合物及其盐和水合物，其中R 1表示任选取代的芳基，任选取代的烷基等; R 2表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基，任选取代的杂环基等; R 3表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基磺酰基，任选取代的杂环基等; R 4和R 5可以相同或不同，表示氢原子，任选取代的烷基或任选取代的烷氧基，或者R 4和R 5可以与相邻氮原子，任选取代的单环或多环; X和Y可以相同或不同，表示每个氧原子或NR 6（其中R 6表示氢原子，任选取代的烷基，任选取代的芳基，任选取代的烷酰基或任选取代的芳酰基）; Z表示氧原子或硫原子; 和波浪线（SIMILAR）表示E异构体，Z异构体或其混合物的构型。

10. 发明申请

WO1998000399A1 NICKEL CATALYZED ADDITION OF -NH- CONTAINING COMPOUNDS TO VINYL AND ARYL HALIDES 审中-公开
标题翻译：含镍化合物的镍催化剂添加到乙烯和芳香族化合物
公开(公告)号：WO1998000399A1
公开(公告)日：1998-01-08
申请号：PCT/US1997011521
申请日：1997-06-30
申请人： E.I. DU PONT DE NEMOURS AND COMPANY , BAKER, Ralph, Thomas , KRISTJANSDOTTIR, Sigrídur, Sóley
发明人： E.I. DU PONT DE NEMOURS AND COMPANY
IPC分类号： C07D209/08
CPC分类号： C07D207/267 , C07C209/08 , C07C231/08 , C07C231/12 , C07D209/52 , C07D211/72 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/22 , C07D277/18 , C07D333/36
摘要： A process for producing unsaturated nitrogen containing compounds such as enamides, enamines and aryl amines/amides is disclosed. A vinyl halide or aryl halide is reacted with an -NH- containing compound in the presence of a catalytic amount of a catalyst precursor composition comprising a zero-valent nickel and an organophosphine or carbene ligand. One step coupling of vinyl halides and aryl halides with -NH- containing compounds is made possible by practice of the invention.
摘要翻译：公开了一种生产不饱和含氮化合物如烯酰胺，烯胺和芳胺/酰胺的方法。在催化量的包含零价镍和有机膦或卡宾配体的催化剂前体组合物的存在下，使乙烯基卤化物或芳基卤化物与含-NH-的化合物反应。乙烯基卤化物和芳基卤化物与含-NH-的化合物的一步耦合是通过实施本发明而实现的。

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