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1. 发明授权

US08653280B2 Process for the preparation of asenapine 有权
标题翻译：制备阿替那平的方法
公开(公告)号：US08653280B2
公开(公告)日：2014-02-18
申请号：US13812212
申请日：2011-07-29
申请人： Pere Dalmases Barjoan , Juan Huguet Clotet , Jordi Peirats Masia
发明人： Pere Dalmases Barjoan , Juan Huguet Clotet , Jordi Peirats Masia
IPC分类号： C07D491/044 , C07D313/14
CPC分类号： C07D313/14 , C07D491/04 , C07D491/044
摘要： The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
摘要翻译：本发明涉及新的式（I）化合物及其制备方法。式（I）的新型化合物可以通过有效的方法转化成阿班那普。本发明还涉及用于该方法的新型中间体及其在制备式（I）化合物中的用途。

2. 发明授权

US08501961B2 HIV protease inhibitors and methods for using 有权
标题翻译： HIV蛋白酶抑制剂和使用方法
公开(公告)号：US08501961B2
公开(公告)日：2013-08-06
申请号：US13002916
申请日：2009-07-08
申请人： Arun K. Ghosh
发明人： Arun K. Ghosh
IPC分类号： C07D487/02 , C07D495/02 , C07D311/94 , A61K31/407 , A61K31/4015 , A61K31/38 , A61K31/35
CPC分类号： C07D493/04 , C07D273/01 , C07D313/14 , C07D319/06 , C07D319/14 , C07D321/06 , C07D321/12 , C07D325/00 , C07D327/10 , C07D491/04 , C07D495/04
摘要： Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.
摘要翻译：描述了抑制人免疫缺陷病毒（HIV）蛋白水解酶的化合物。还描述了抑制剂的制备，含有它们的药物组合物，以及化合物或组合物用于治疗HIV感染的用途。

3. 发明授权

US07288543B2 Opioid receptor antagonists 有权
标题翻译：阿片受体拮抗剂
公开(公告)号：US07288543B2
公开(公告)日：2007-10-30
申请号：US10598690
申请日：2005-03-08
申请人： Howard Barff Broughton , Nuria Diaz Buezo , Charles Howard Mitch , Concepcion Pedregal-Tercero
发明人： Howard Barff Broughton , Nuria Diaz Buezo , Charles Howard Mitch , Concepcion Pedregal-Tercero
IPC分类号： A01N43/58 , A01N43/54 , A61K31/335 , C07D239/00 , C07D491/00
CPC分类号： C07D307/91 , C07D313/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D491/04
摘要： A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3′, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
摘要翻译：式（I）（I）的化合物，其中包括R3'，E，p，j，y，z，A，B和C的变量X1至X6，Ra，Rb，R1至R7如上所述或药学上公开了可用于治疗，预防或改善肥胖症和相关疾病的盐，溶剂合物，对映异构体，外消旋物，非对映体或其混合物

4. 发明申请

US20040127713A1 Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
标题翻译：三环稠合杂环化合物，其制备方法及其应用
公开(公告)号：US20040127713A1
公开(公告)日：2004-07-01
申请号：US10727644
申请日：2003-12-05
申请人： Nippon Suisan Kaisha, Ltd.
发明人： Shuji Jinno , Takaaki Okita , Naomi Ohtsuka , Shinya Yamashita , Junichiro Hata , Jiro Takeo
IPC分类号： C07D498/02 , C07D491/02
CPC分类号： C07D405/04 , A61K31/31 , A61K31/335 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/4353 , A61K31/4427 , C07D313/14 , C07D337/14 , C07D407/04 , C07D409/04 , C07D491/04
摘要： Compounds represented by formula (1), 1 wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRRnull (wherein R and Rnull are the same as the above defined R); Y is, for example, CH, CH2 or CnullO; Z is, for example, O, S, SnullO or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.
摘要翻译：由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述相同定义R）; Y为例如CH，CH 2或C = O; Z是例如O，S，S = O或SO 2; U是C或N; R 1至R 4各自独立地为例如氢原子，OR，SR（其中R与上述定义相同），或芳香环，取代的芳环或杂环; R5和R8中的至少一个是例如OH，并且R5和R8的剩余部分各自独立地为例如氢原子或OH，其光学异构体，其缀合物或其药学上可接受的盐。这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

5. 发明申请

US20030065021A1 Tracheal smooth muscle relaxants 审中-公开
标题翻译：气管平滑肌松弛剂
公开(公告)号：US20030065021A1
公开(公告)日：2003-04-03
申请号：US10260355
申请日：2002-10-01
发明人： Shinya Yamashita , Jiro Takeo , Shuji Jinno , Yasuyo Kogure , Hiroyuki Onuki , Takaaki Okita , Junichiro Hata , Yasuhiro Fukuda , Naomi Ohtsuka
IPC分类号： C07D327/00 , C07D341/00 , A61K031/38 , A61K031/335
CPC分类号： C07D337/14 , A61K31/352 , A61K31/382 , C07D313/14 , Y10S514/826
摘要： The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient. 1 nullIn the formula, X and Y each is any group selected from a group consisting of CH2, CHW1 (where W1 is halogen atom, hydroxyl group or lower alkoxy group) and CnullO when the bond of X and Y is a single bond while, when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW2 (where W2 is lower alkyl group or lower alkylcarbonyl group); Z is O, S, SnullO or SO2; and R1nullR8 each is selected from a group consisting of hydrogen atom, VR9 (where V is O, S, SnullO or SO2; and R9 is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl groupnull.
摘要翻译：本发明提供含有下述式（1）表示的化合物或其药理学可接受的盐作为有效成分的气管平滑肌松弛剂。 [式中，X和Y分别是选自由CH 2，CHW 1（其中，W 1为卤素原子，羟基或低级烷氧基）和C = O的任何基团，X和Y的键为单键时而当它是双键时，X和Y各自是选自CH和COW 2（其中W 2是低级烷基或低级烷基羰基）的任何基团; Z是O，S，S = O或SO 2; 并且R 1〜R 8各自选自氢原子，VR9（其中V为O，S，S = O或SO 2; R 9为氢原子，低级烷基，羟基低级烷基，低级酰基，三卤甲基羧基低级烷基，羟基低级烷基，羟基低级烯基，羟基低级炔基，卤素原子，低级烷基，低级烷基酮，三卤代甲基，三甲基甲硅烷基乙炔基，硝基，氨基， N-羰基低级烷基，低级烷基苯基和苯基]。

6. 发明授权

US06498190B1 Bicyclic amino derivatives and PGD2 antagonist containing the same 失效
标题翻译：双环氨基衍生物和含有相同的PGD2拮抗剂
公开(公告)号：US06498190B1
公开(公告)日：2002-12-24
申请号：US09506606
申请日：2000-02-18
申请人： Mitsuaki Ohtani , Akinori Arimura , Tatsuo Tsuri , Junji Kishino , Tsunetoshi Honma
发明人： Mitsuaki Ohtani , Akinori Arimura , Tatsuo Tsuri , Junji Kishino , Tsunetoshi Honma
IPC分类号： C07C40500
CPC分类号： C07D213/81 , A61K31/557 , C07C233/52 , C07C233/63 , C07C233/74 , C07C233/81 , C07C233/84 , C07C235/22 , C07C235/36 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C245/08 , C07C251/48 , C07C251/86 , C07C255/57 , C07C271/24 , C07C275/42 , C07C281/14 , C07C309/65 , C07C311/13 , C07C311/20 , C07C311/29 , C07C311/37 , C07C311/43 , C07C311/46 , C07C311/51 , C07C317/44 , C07C323/62 , C07C337/08 , C07C2601/14 , C07C2601/16 , C07C2602/42 , C07C2603/18 , C07D207/34 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/88 , C07D213/56 , C07D215/36 , C07D221/12 , C07D231/12 , C07D233/56 , C07D235/06 , C07D249/08 , C07D257/04 , C07D261/18 , C07D263/57 , C07D271/06 , C07D271/107 , C07D275/03 , C07D277/20 , C07D277/56 , C07D279/20 , C07D279/22 , C07D285/06 , C07D285/12 , C07D295/192 , C07D307/68 , C07D307/84 , C07D307/91 , C07D311/12 , C07D311/24 , C07D311/82 , C07D313/14 , C07D317/48 , C07D319/24 , C07D333/18 , C07D333/24 , C07D333/32 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D333/68 , C07D333/76 , C07D333/78 , C07D337/14 , C07F9/5355
摘要： A compound of the formula (I): wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1—X2—X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
摘要翻译：式（I）的化合物：其中例如下列化合物：其中R 1是CH 3，H或Na; X1-X2-X3等同于其盐或其水合物可用作PGD2拮抗剂，可用作治疗涉及肥大细胞功能障碍的疾病的药物，例如系统性肥大细胞增多症和系统性肥大细胞活化的紊乱，以及气管收缩，哮喘，过敏性鼻炎，过敏性结膜炎，荨麻疹，由缺血再灌注引起的损伤，以及作为抗炎剂。它在治疗鼻塞方面特别有用。

7. 发明授权

US06495592B1 Tracheal smooth muscle relaxants 失效
标题翻译：气管平滑肌松弛剂
公开(公告)号：US06495592B1
公开(公告)日：2002-12-17
申请号：US09609310
申请日：2000-06-30
申请人： Shinya Yamashita , Jiro Takeo , Shuji Jinno , Yasuyo Kogure , Hiroyuki Onuki , Takaaki Okita , Junichiro Hata , Yasuhiro Fukuda , Naomi Ohtsuka
发明人： Shinya Yamashita , Jiro Takeo , Shuji Jinno , Yasuyo Kogure , Hiroyuki Onuki , Takaaki Okita , Junichiro Hata , Yasuhiro Fukuda , Naomi Ohtsuka
IPC分类号： A61K31335
CPC分类号： C07D337/14 , A61K31/352 , A61K31/382 , C07D313/14 , Y10S514/826
摘要： The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.
摘要翻译：本发明提供含有下述式（1）表示的化合物或其药理学可接受的盐作为有效成分的气管平滑肌松弛剂。

8. 发明授权

US4837227A Aminoalkylthiodibenzoxepins and pharmaceutical use 失效
标题翻译：氨基烷基硫代二苯并氧氮皮素和药物用途
公开(公告)号：US4837227A
公开(公告)日：1989-06-06
申请号：US738507
申请日：1985-05-28
申请人： Helen H. Ong , Vernon B. Anderson , James A. Profitt
发明人： Helen H. Ong , Vernon B. Anderson , James A. Profitt
IPC分类号： C07D313/14
CPC分类号： C07D313/14
摘要： Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
摘要翻译：公开了新的氨基烷基硫代二氧化硫蛋白，其生理上可耐受的酸加成盐，其制备方法，包括其的药物和兽医制剂以及通过施用方法进行治疗。这些化合物可用作镇痛药，抗抑郁药和抗惊厥药。还公开了一种通过碱金属在低级烷醇中选择性还原烯烃的方法。

9. 发明授权

US4105664A Dibenz[b,f]oxepin derivatives 失效
标题翻译： DIBENZ（B，F）OXEPIN衍生物
公开(公告)号：US4105664A
公开(公告)日：1978-08-08
申请号：US779196
申请日：1977-03-18
申请人： Max Gerecke , Emilio Kyburz , Jean-Pierre Kaplan
发明人： Max Gerecke , Emilio Kyburz , Jean-Pierre Kaplan
IPC分类号： C07D313/14 , C07D405/04 , C07D405/14 , C07D413/14
CPC分类号： C07D405/04 , C07D313/14 , C07D405/14 , C07D413/14
摘要： Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.

10. 发明授权

US4104280A Dibenzo [b.f]thiepin and dibenzo[b.f]oxepin derivatives 失效
标题翻译： Dibenzo {8b.f {9 thiepin and dibenzo {8b.f {9 oxepin derivatives
公开(公告)号：US4104280A
公开(公告)日：1978-08-01
申请号：US765493
申请日：1977-02-04
申请人： Jack Ackrell
发明人： Jack Ackrell
IPC分类号： C07C41/26 , C07D313/14 , C07D337/14
CPC分类号： C07C323/00 , C07C41/26 , C07D313/14 , C07D337/14
摘要： Novel dibenzo[b.f]thiepin and oxepin compounds of the formula and the pharmaceutically acceptable esters and salts thereof, wherein R is hydrogen or methyl; X is oxygen or S(O).sub.n in which n is the integer 0, 1 or 2 and Z is a single or double bond, provided that when Z is a double bond X is not SO, and when R is methyl the compounds are (dl) mixtures, and methods for the production thereof.
摘要翻译：新颖的二苯并[b.f]硫酮和式（Ⅱ）化合物及其药学上可接受的酯和盐，其中R是氢或甲基; X是氧或S（O）n，其中n是整数0,1或2，Z是单键或双键，条件是当Z是双键时X不是SO，当R是甲基时，化合物是（dl）混合物及其生产方法。

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