公开(公告)号：US20090163461A1

公开(公告)日：2009-06-25

申请号：US11887580

申请日：2006-03-31

申请人： Kazuhiro Shiba ,  Kiichi Ishiwata ,  Hideo Tsukada ,  Shingo Nishiyama

发明人： Kazuhiro Shiba ,  Kiichi Ishiwata ,  Hideo Tsukada ,  Shingo Nishiyama

IPC分类号： A61K31/555 ,  C07D211/22 ,  C07F15/00 ,  A61K31/445

CPC分类号： C07D211/14 ,  A61K51/0457 ,  C07B59/002 ,  C07F7/2208

摘要： The present invention provides a novel compound represented by the formula (I): wherein R1 and R2 are as defined in the specification, or a salt thereof, which is useful as a reagent (radiotracer) for VAChT mapping and the like, and can be used for positron emission tomography (PET), and a production method of the compound. Moreover, the present invention provides a diagnostic reagent for diagnosing cholinergic neurodegenerative disorders (e.g., Alzheimer's disease, memory disorder, learning disorder, schizophrenia, cognitive dysfunction, hyperactivity disorder, anxiety neurosis, depression, analgia, Parkinson's disease and the like) and the like, which contains the aforementioned compound.

摘要翻译： 本发明提供由式（I）表示的新化合物：其中R1和R2如说明书中所定义，或其盐，其用作VAChT作图等的试剂（放射性示踪剂），并且可以是 用于正电子发射断层摄影（PET），以及该化合物的制备方法。 此外，本发明提供了用于诊断胆碱能神经变性疾病（例如阿尔茨海默病，记忆障碍，学习障碍，精神分裂症，认知功能障碍，多动障碍，焦虑性神经症，抑郁，肛门痛，帕金森病等）的诊断试剂， ，其含有上述化合物。

公开(公告)号：US20080171881A1

公开(公告)日：2008-07-17

申请号：US11885125

申请日：2006-03-22

申请人： Naruhisa Hirai ,  Jun Kuwana

发明人： Naruhisa Hirai ,  Jun Kuwana

IPC分类号： C07D211/22 ,  C07C233/00 ,  C07D233/40 ,  C07D249/12

CPC分类号： C07D251/32 ,  Y02P20/55

摘要： It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity.Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.

摘要翻译： 期望提供一种通过催化具有二羧酰亚胺骨架的化合物从反应产物中容易地除去催化剂衍生的杂质的方法，从而有效地产生高纯度的目标化合物。 公开了一种在催化剂存在下通过底物的反应制备有机化合物的方法，所述催化剂包括具有由下式（i）表示的二羧酰亚胺骨架的化合物：其中R表示氢原子或羟基保护基 。 该方法包括用热水处理反应产物以分解和除去由催化剂衍生的杂质的步骤。 热水的温度优选为100℃以上。

公开(公告)号：US20080090839A1

公开(公告)日：2008-04-17

申请号：US11832816

申请日：2007-08-02

申请人： Vincent Sandanayaka ,  Pushpa Chandrasekar ,  Mark Gurney

发明人： Vincent Sandanayaka ,  Pushpa Chandrasekar ,  Mark Gurney

IPC分类号： A61K31/495 ,  A61K31/40 ,  A61P29/00 ,  C07D211/22 ,  C07D295/033 ,  C07D207/06 ,  A61K31/4453

CPC分类号： C07D207/08 ,  C07D295/088 ,  C07D295/15

摘要： A chemical genus of biphenyl heterocycle derivative inhibitors of LTA4H (leukotriene A4 hydrolase) of the formula: is disclosed. In these compounds Q and Z are (CH2)1-10; in which one or two (CH2) may optionally be replaced by —O—, —NR1—, —SO—, —S(O)2—, —C(═O)— or —C═O(NH)—; Het is a 5-7 membered non-aromatic nitrogen heterocycle; and W is acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, —COOalkyl, —CHO, heterocyclyl, substituted aryl, or substituted heterocyclyl, or taken together ZW can be H or —COOalkyl. The compounds are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

摘要翻译： 公开了具有下式的LTA4H（白三烯A4水解酶）的联苯基杂环衍生物抑制剂的化学属。 在这些化合物中，Q和Z是（CH 2）2 - 其中一个或两个（CH 2）2可以任选地被-O-，-NR 1 - ， - SO - ， - S（O）2 -C（ - ） - 或-CO（NH） - ; Het是5-7元非芳族氮杂环; 并且W是酰基，羟基，羧基，氨基，甲酰氨基，氨酰基，-COO烷基，-CHO，杂环基，取代的芳基或取代的杂环基，或一起ZW可以是H或-COO烷基。 该化合物可用于治疗和预防和预防炎性疾病和病症。

公开(公告)号：US07247730B2

公开(公告)日：2007-07-24

申请号：US10793080

申请日：2004-03-04

申请人： Arie Gutman ,  Igor Zaltsman ,  Anton Shalimov ,  Maxim Sotrihin ,  Gennady Nisnevich ,  Lev Yudovich ,  Irina Fedotev

发明人： Arie Gutman ,  Igor Zaltsman ,  Anton Shalimov ,  Maxim Sotrihin ,  Gennady Nisnevich ,  Lev Yudovich ,  Irina Fedotev

IPC分类号： C07D211/22

CPC分类号： C07D211/34

摘要： The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.

摘要翻译： 本发明提供了一种用于制备具有高光学纯度的右哌醋酸盐酸盐的新型和有效的方法，该方法包括：（a）使苏氨酸-N-Boc-色氨酸与（S）-1-苯基乙胺的溶液，分离 （R，R）富含N-Boc-异戊酸的沉淀固体盐与（S）-1-苯乙基胺在反应混合物中的沉淀，并重结晶，再沉淀和/或研磨所述盐; （b）将步骤（a）中得到的（R，R）-N-Boc-异戊酸和（S）-1-苯基乙胺的固体盐与酸水溶液和（R，R）-N-Boc-活化后 酸从混合物中; 和（c）使步骤（b）中制备的（R，R）-N-Boc-异戊酸与氯化氢和甲醇反应，得到光学纯度为至少99％ee的盐酸偏苯甲酸酯。 本发明进一步提供（R，R）-N-Boc-异戊酸与（S）-1-苯基乙胺的盐作为制备右哌甲酯盐酸盐的新中间体。

公开(公告)号：US20070066652A1

公开(公告)日：2007-03-22

申请号：US10557067

申请日：2004-05-13

申请人： William Brown ,  Andrew Griffin

发明人： William Brown ,  Andrew Griffin

IPC分类号： A61K31/453 ,  A61K31/452 ,  A61K31/445 ,  C07D211/22 ,  C07D409/02 ,  C07D405/02

CPC分类号： C07D405/06 ,  C07D211/70 ,  C07D411/06

摘要： Compounds of general formula: Formula (I) wherein R1, R2, R3 and A are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

摘要翻译： 通式为其中R 1，R 2，R 3和A的式（I）的化合物如说明书中所定义 作为其盐，对映体和包括该化合物的药物组合物。 它们可用于治疗，特别是治疗疼痛。

公开(公告)号：US07138524B2

公开(公告)日：2006-11-21

申请号：US10162011

申请日：2002-06-03

申请人： Frederick J. McCarty ,  Albert A. Carr

发明人： Frederick J. McCarty ,  Albert A. Carr

IPC分类号： C07D211/22

CPC分类号： A61K31/445 ,  C07D211/22

摘要： The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.

公开(公告)号：US20050282858A1

公开(公告)日：2005-12-22

申请号：US11122309

申请日：2005-05-04

申请人： Wenqing Yao ,  Jincong Zhuo ,  Meizhong Xu ,  Brian Metcalf ,  Chunhong He ,  Ding-Quan Qian ,  Colin Zhang

发明人： Wenqing Yao ,  Jincong Zhuo ,  Meizhong Xu ,  Brian Metcalf ,  Chunhong He ,  Ding-Quan Qian ,  Colin Zhang

IPC分类号： A61K31/401 ,  A61K31/445 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/263 ,  C07D207/30 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/62 ,  C07D209/70 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/48 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/66 ,  C07D211/70 ,  C07D213/38 ,  C07D217/06 ,  C07D217/26 ,  C07D221/00 ,  C07D221/20 ,  C07D223/02 ,  C07D223/04 ,  C07D231/04 ,  C07D295/185 ,  C07D333/34 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/20 ,  C07D493/10 ,  C07D495/04 ,  C07D498/20 ,  C07D513/10

CPC分类号： C07D207/06 ,  A61K31/407 ,  A61K31/4439 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/62 ,  C07D209/70 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/48 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/66 ,  C07D211/70 ,  C07D213/38 ,  C07D217/06 ,  C07D217/26 ,  C07D221/20 ,  C07D295/185 ,  C07D333/34 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D493/10 ,  C07D495/04 ,  C07D498/20 ,  C07D513/10

摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

公开(公告)号：US06974872B2

公开(公告)日：2005-12-13

申请号：US10212854

申请日：2002-08-05

申请人： Thomas E. D'Ambra ,  Garry M. Pilling

发明人： Thomas E. D'Ambra ,  Garry M. Pilling

IPC分类号： A61K31/00 ,  A61K31/42 ,  A61K31/421 ,  A61K31/445 ,  A61P37/00 ,  A61P37/08 ,  C07D211/22 ,  C07D211/54 ,  C07D261/04 ,  C07D263/10 ,  C07D211/14 ,  C07D419/10

CPC分类号： C07D211/54 ,  C07D211/22 ,  C07D261/04

摘要： The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

摘要翻译： 本发明公开了制备下式的哌啶衍生物化合物的方法：其中n为0或1; R 1是氢或羟基; R 2是氢; 或者当n为0时，R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键 > 2 ，条件是当n为1时，R 1和R 2各自为氢; R 3是-COOH或-COOR 4; R 4是烷基或芳基部分; A，B和D是它们的环的取代基，其各自可以不同或相同，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。

公开(公告)号：US06969724B2

公开(公告)日：2005-11-29

申请号：US10324571

申请日：2002-12-19

申请人： Daniela Barlocco ,  Giorgio Cignarella ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Silvano Ronzoni

发明人： Daniela Barlocco ,  Giorgio Cignarella ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Silvano Ronzoni

IPC分类号： A61K31/451 ,  A61P1/16 ,  A61P5/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P43/00 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  A61K31/445

CPC分类号： C07D211/18 ,  C07D211/14 ,  C07D211/22

摘要： Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl or C1-6alkoxy groups are unsubstituted or substituted one or more times by halo, which aryl group is unsubstituted or substituted one or more times by aryl, heterocyclyl, aryloxy, arylC1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkyl, hydroxy, C1-6alkenoxy, C1-6alkoxy, halo, or C1-6alkyl, which C1-6alkyl may be substituted one or more times by halo, and which aryl group is linked to said ring by a single bond or is benzo-condensed therewith are ligands of the ORL-1 receptor.

公开(公告)号：US06951874B2

公开(公告)日：2005-10-04

申请号：US10204754

申请日：2001-02-23

申请人： Peter Hansen ,  Lars Pettersson

发明人： Peter Hansen ,  Lars Pettersson

IPC分类号： C07D211/18 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/435 ,  A61K31/437 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/4523 ,  A61K31/454 ,  A61P1/00 ,  A61P1/04 ,  A61P3/10 ,  A61P3/14 ,  A61P5/14 ,  A61P5/16 ,  A61P7/00 ,  A61P7/04 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P17/08 ,  A61P17/14 ,  A61P17/16 ,  A61P19/00 ,  A61P19/02 ,  A61P19/04 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/08 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D207/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D209/08 ,  C07D211/06 ,  C07D211/22 ,  C07D211/32 ,  C07D211/36 ,  C07D211/46 ,  C07D211/58 ,  C07D295/08 ,  C07D295/092 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

CPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D295/088 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

摘要： The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy

摘要翻译： 本发明提供通式（I）的化合物，其中Q，R，R 2，R 4，R 5，R 6， R＆lt; 7＆gt;和＆lt; 8＆gt;如本说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途