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1. 发明授权

US09573934B2 Methods and compositions for the synthesis of multimerizing agents 有权
标题翻译：用于合成多聚化剂的方法和组合物
公开(公告)号：US09573934B2
公开(公告)日：2017-02-21
申请号：US14607831
申请日：2015-01-28
申请人： ARIAD Pharmaceuticals, Inc.
发明人： Feng Li , Yihan Wang
IPC分类号： C07D211/60 , C07C51/06 , C07C209/08 , C07C231/02 , C07C235/34 , C07D205/04 , C07D319/06 , C07D401/12 , C07D319/04 , C07B53/00 , C07C209/62 , C07C209/74 , C07C231/18
CPC分类号： C07D401/12 , C07B53/00 , C07B2200/07 , C07C51/06 , C07C209/08 , C07C209/62 , C07C209/74 , C07C231/02 , C07C231/18 , C07C235/34 , C07D205/04 , C07D211/60 , C07D319/04 , C07D319/06 , C07C211/15 , C07C211/13 , C07C235/20 , C07C59/64
摘要： The invention features methods and compositions for the synthesis of multimerizing agents.
摘要翻译：本发明的特征在于用于合成多聚化剂的方法和组合物。

2. 发明授权

US08252306B2 Process for preparing a semi-solid delivery vehicle comprising granisetron 有权
标题翻译：制备包含格拉司琼的半固体递送载体的方法
公开(公告)号：US08252306B2
公开(公告)日：2012-08-28
申请号：US13279949
申请日：2011-10-24
申请人： Steven Y. Ng , Hui Rong Shen , Jorge Heller
发明人： Steven Y. Ng , Hui Rong Shen , Jorge Heller
IPC分类号： A61K31/439 , A61K31/435 , A61K31/46 , A61K31/416 , A61K47/30 , A61P1/08 , C07D319/04
CPC分类号： A61K47/34 , A61K8/85 , A61K8/86 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/06 , A61K9/1647 , A61K31/439 , A61K31/445 , A61K31/573 , A61K31/765 , A61K45/06 , A61K47/10 , A61Q15/00 , A61Q17/04 , A61Q19/00
摘要： A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
摘要翻译：半固体递送载体含有聚原酸酯和赋形剂，半固体药物组合物含有活性剂和递送载体。药物组合物可以是局部，注射剂或可注射制剂; 并适用于活性剂的局部递送。还公开了治疗方法。

3. 发明申请

US20100217018A1 Method for the Production of Substituted and Unsubstituted Cyclohexanone Monoketals 审中-公开
标题翻译：取代和未取代的环己酮单酮的制备方法
公开(公告)号：US20100217018A1
公开(公告)日：2010-08-26
申请号：US12738316
申请日：2008-10-16
申请人： Wahed Ahmed Moradi , Matthias Decker , Gunter Karig , Thomas Himmler , Norbert Lui , Alexander Straub
发明人： Wahed Ahmed Moradi , Matthias Decker , Gunter Karig , Thomas Himmler , Norbert Lui , Alexander Straub
IPC分类号： C07D319/04 , C07D317/72 , C07C45/00
CPC分类号： C07C45/62 , C07C45/673 , C07C2601/14 , C07D317/72 , C07D319/08 , C25B3/04 , C07C49/517 , C07C49/753
摘要： The invention relates to a novel process for preparing and isolating known substituted and unsubstituted 1,4-cyclohexanone monoketals.
摘要翻译：本发明涉及制备和分离已知的取代和未取代的1,4-环己酮单酮的新方法。

4. 发明申请

US20090137530A1 Amine Compound and Use Thereof for Medical Purposes 有权
标题翻译：胺化合物及其用途用于医疗用途
公开(公告)号：US20090137530A1
公开(公告)日：2009-05-28
申请号：US12086419
申请日：2006-12-15
申请人： Masatoshi Kiuchi , Kaoru Marukawa , Nobutaka Kobayashi , Kunio Sugahara
发明人： Masatoshi Kiuchi , Kaoru Marukawa , Nobutaka Kobayashi , Kunio Sugahara
IPC分类号： A61K31/137 , C07D319/04 , C07C217/64 , C07C271/16 , C07F9/09 , A61P37/00 , A61P3/10 , A61P25/00 , A61K31/661 , C07D309/12 , A61K31/351 , A61K31/27
CPC分类号： C07C235/34 , C07C217/64 , C07C235/78 , C07C255/54 , C07C271/16 , C07C323/32 , C07C323/43 , C07D319/06 , C07F7/1804 , C07F9/09 , C07F9/091 , C07F9/141 , C07F9/4056 , C07F9/6527 , C07F9/653
摘要： A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(═O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH═CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
摘要翻译：由下式（I）表示的新型胺化合物，其免疫抑制作用优异，排斥抑制作用等，并且显示降低的副作用，例如心动过缓等，或其药学上可接受的酸加成盐或水合物或溶剂合物，以及含有该化合物和药学上可接受的载体的药物组合物。其中R为氢原子或P（-O）（OH）2，X为氧原子或硫原子，Y为CH 2 CH 2或CH-CH，R 1为氰基或碳数为1至4的烷基，通过卤素原子，R 2是碳数为1至4的烷基，并且任选地被羟基或卤素原子取代，R 3和R 4可以相同或不同，各自为氢原子或碳数为1至4的烷基，n为5-8。

5. 发明申请

US20020068758A1 Novel orally active iron (III) chelators 有权
标题翻译：新型口服活性铁（III）螯合剂
公开(公告)号：US20020068758A1
公开(公告)日：2002-06-06
申请号：US09944113
申请日：2001-09-04
申请人： BTG International Limited.
发明人： Robert Charles Hider , Gary Stuart Tilbrook , Zudong Liu
IPC分类号： A61K031/357 , C07D319/04
CPC分类号： C07D213/69 , C07D213/81 , C07D309/40 , C07D417/06 , C07D493/04
摘要： A novel 3-hydroxypyridinone compound of formula I is provided 1 wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6 -aryloxy or C7-10 aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2 ; characterized in that R2 is selected from groups (i) nullCONHnullR5 (ii) nullCH2NHCOnullR5 (iii) nullSO2NHnullR5 (iv) nullCH2NHSO2nullR5 (v) nullCR6R6OR7 (viii) nullCONHCOR5 wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl or a pharmaceutically acceptable salt of any such compound with the proviso that when R7 is hydrogen, R6 is not selected from aryl and with the proviso that the compound is not 1-ethyl-2-(1null-hydroxyethyl)-3-hydroxypyridin-4-one.
摘要翻译：提供式I的新颖的3-羟基吡啶酮化合物，其中R是氢或通过体内代谢除去以提供游离羟基化合物的基团，R 1是脂族烃基或被羟基取代的脂族烃基或羧酸酯，磺酸酯或C 1-6烷氧基，C 6芳氧基或C 7-10芳烷氧基醚，R 3选自氢和C 1-6烷基; 并且R 4选自氢，C 1-6烷基和如对于R 2所述的基团; 其特征在于R2选自基团（ⅰ）-CONH-R5（ⅱ）-CH2NHCO-R5（ⅲ）-SO2NH-R5（ⅳ）-CH2NHSO2-R5（ⅴ）-CR6R6OR7（ii）-CONHCOR5，其中选择R5 由氢和任选的羟基，烷氧基或芳烷氧基取代的C 1-13烷基，芳基和C 7-13芳烷基，R 6独立地选自氢，C 1-13烷基，芳基和C 7-13芳烷基，并且R 7选自氢，C 1 -13烷基，芳基和C7-13芳烷基或任何此类化合物的药学上可接受的盐，条件是当R7为氢时，R6不选自芳基，条件是该化合物不是1-乙基-2-（ 1'-羟乙基）-3-羟基吡啶-4-酮

6. 发明授权

US5489691A Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis 失效
标题翻译：用于反式-6-（2-（取代 - 吡咯-1-基）烷基）吡喃-2-酮胆固醇合成抑制剂的方法
公开(公告)号：US5489691A
公开(公告)日：1996-02-06
申请号：US440796
申请日：1995-05-15
申请人： Donald E. Butler , Tung Van Le , Thomas N. Nanninga
发明人： Donald E. Butler , Tung Van Le , Thomas N. Nanninga
IPC分类号： C07D295/18 , A61K31/40 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/445 , A61P3/06 , C07C255/20 , C07C255/26 , C07C255/27 , C07D207/06 , C07D207/325 , C07D207/34 , C07D211/10 , C07D211/16 , C07D265/30 , C07D319/04 , C07D319/06 , C07D401/06 , C07D405/02 , C07D405/06 , C07D405/14 , C07D491/113
CPC分类号： C07D405/06 , C07D207/34
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.
摘要翻译：描述了通过新的合成制备反式-6- [2-（取代 - 吡咯-1-基）烷基]吡喃-2-酮的改进方法，其中将α-金属化的N，N-二取代的乙酰胺转化为七具体而言，制备（2R-反式）-5-（4-氟苯基）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢-4 - 羟基-6-氧代-2H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺以及生物转化为降血脂和降血胆固醇剂的方法和前药中使用的其它有价值的中间体和药物组合物一样。

7. 发明授权

US5298627A Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis 失效
标题翻译：反式-6- [2-（取代 - 吡咯-1-基）烷基]吡喃-2-酮胆固醇合成抑制剂的方法
公开(公告)号：US5298627A
公开(公告)日：1994-03-29
申请号：US025701
申请日：1993-03-03
申请人： Donald E. Butler , Tung V. Le , Thomas N. Nanninga
发明人： Donald E. Butler , Tung V. Le , Thomas N. Nanninga
IPC分类号： C07D295/18 , A61K31/40 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/445 , A61P3/06 , C07C255/20 , C07C255/26 , C07C255/27 , C07D207/06 , C07D207/325 , C07D207/34 , C07D211/10 , C07D211/16 , C07D265/30 , C07D319/04 , C07D319/06 , C07D401/06 , C07D405/02 , C07D405/06 , C07D405/14 , C07D491/113 , C07D207/323 , C07D309/10
CPC分类号： C07D405/06 , C07D207/34
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.
摘要翻译：描述了通过新的合成制备反式-6- [2-（取代 - 吡咯-1-基）烷基]吡喃-2-酮的改进方法，其中将α-金属化的N，N-二取代的乙酰胺转化为七具体而言，制备（2R-反式）-5-（4-氟苯基）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢 - 4-羟基-6-氧代-2H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺以及生物转化为降血脂和低胆固醇血症药物和药物组合物的方法和前药中使用的其它有价值的中间体一样的。

8. 发明授权

US5256689A Cholesterol lowering compounds 失效
标题翻译：胆固醇降低化合物
公开(公告)号：US5256689A
公开(公告)日：1993-10-26
申请号：US966764
申请日：1992-10-26
申请人： Yuan-Ching P. Chiang
发明人： Yuan-Ching P. Chiang
IPC分类号： C07D493/08 , C07H19/01 , A61K31/335 , C07D319/04
CPC分类号： C07D493/08 , C07H19/01
摘要： Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.
摘要翻译：本文公开了结构式（I）化合物（I），其可用作降胆固醇剂和角鲨烯合酶抑制剂。

9. 发明授权

US4769479A Hydroxyphenylpropionic acid ester with novel crystalline structure and production thereof 失效
标题翻译：羟基苯基丙酸酯，具有新颖的晶体结构及其制备
公开(公告)号：US4769479A
公开(公告)日：1988-09-06
申请号：US868743
申请日：1986-05-30
申请人： Manji Sasaki , Chinehito Ebina , Haruki Okamura , Shinichi Yachigo , Tamaki Ishii
发明人： Manji Sasaki , Chinehito Ebina , Haruki Okamura , Shinichi Yachigo , Tamaki Ishii
IPC分类号： C07D493/10 , C07D319/04
CPC分类号： C07D493/10
摘要： 3,9-bis{2-[3-(3-tert-butyl-4-hydroxy-5-methylphenyl) propionyloxy]-1,1-dimethylethyl}-2,4,8,10-tetraoxaspiro[5.5] undecane having a novel crystalline structure which, when subjected to Cu-K.sub..alpha. X-ray diffraction, shows sharp X-ray diffraction peaks at angles of diffraction, 2.theta.=4.2.degree. and 2.theta.=10.6.degree.. Also provided is a method for producing this compound.
摘要翻译： 3,9-双{2- [3-（3-叔丁基-4-羟基-5-甲基苯基）丙酰氧基] -1,1-二甲基乙基} -2,4,8,10-四氧杂螺[5.5]十一烷，其具有当经受Cu-Kαα射线衍射时，在衍射角2θ= 4.2°和2θ= 10.6°处显示出尖锐的X射线衍射峰。还提供了该化合物的制造方法。

10. 发明授权

US4567197A 1,3-Dioxan-5-ylalkenoic acids 失效
标题翻译： 1,3-二恶烷-5-基链烯酸
公开(公告)号：US4567197A
公开(公告)日：1986-01-28
申请号：US492247
申请日：1983-05-06
申请人： Andrew G. Brewster , Peter W. R. Caulkett
发明人： Andrew G. Brewster , Peter W. R. Caulkett
IPC分类号： C07D319/06 , A61K31/335 , A61K31/35 , A61K31/357 , A61K31/36 , A61P7/02 , A61P9/08 , A61P9/12 , A61P11/08 , A61P43/00 , C07C20060101 , C07C59/48 , C07C69/732 , C07D309/06 , C07D317/54 , C07D319/04 , C07D319/08 , C07D325/00 , C07D407/04 , C07D407/10 , C07D413/06
CPC分类号： C07D319/08 , C07D319/06 , C07D407/04
摘要： The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.
摘要翻译：本发明涉及式I的4-苯基-1,3-二恶烷-5-基亚烯基酸衍生物，其在二恶烷环的4和5位具有顺式相对立体化学，其中Ra和Rb分别为氢，烷基，卤代烷基，烯基和任选取代的芳基或芳基烷基，R c是羟基，烷氧基或烷基磺酰胺基，n是1或2，A是亚乙基或亚乙烯基，Y是任选被烷基取代的（2-5C）聚亚甲基，苯环B是任选取代的苯基，或当Rc为羟基时，其盐。酸衍生物拮抗血栓素A2（TXA2）的一种或多种作用，并且预期在涉及TXA2的那些疾病状况下具有价值。本发明还提供含有式I酸衍生物的药物组合物及其化学生产方法。

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