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21. 发明授权

US5486528A Basic ethers and process for the preparation thereof 失效
标题翻译：碱性醚及其制备方法
公开(公告)号：US5486528A
公开(公告)日：1996-01-23
申请号：US226089
申请日：1994-04-11
申请人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Eva Schmidt , Andras Egyed , Marton Fekete , Istvan Gacsalyi , Istvan Gyertyan , Tibor Mezei , Kalara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Enik Szirt nee Kiszelly
发明人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Eva Schmidt , Andras Egyed , Marton Fekete , Istvan Gacsalyi , Istvan Gyertyan , Tibor Mezei , Kalara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Enik Szirt nee Kiszelly
IPC分类号： A61K31/135 , A61K31/15 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/495 , A61P1/04 , A61P25/20 , C07C251/32 , C07C251/58 , C07D207/08 , C07D213/30 , C07D295/00 , C07D295/08 , C07D295/088 , C07D317/58 , C07D405/12 , C07C251/48
CPC分类号： C07D207/08 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/14
摘要： Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.
摘要翻译：新型通式（I）的基本醚，其中R 1和R 2独立地为氢，卤素或C 1-4烷氧基，或一起它们代表3,4-亚甲二氧基，R代表C1-8烷基，R3代表氢，C1-4烷基或羟基，A是价键或亚甲基，R4和R5独立地是氢，C1-12烷基或C1-12烯基，或R4和R5与相邻的氮原子1一起形成吡咯烷基，1-哌啶基，吗啉代或1-哌嗪基，立体和旋光异构体及其可能的混合物，其酸加成盐和季铵衍生物。碱性醚具有抗溃疡和抗焦虑作用。

22. 发明授权

US5439940A Benz[e]indene derivatives 失效
标题翻译：苯并[e]茚衍生物
公开(公告)号：US5439940A
公开(公告)日：1995-08-08
申请号：US141954
申请日：1993-10-28
申请人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
发明人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/16 , A61K31/335 , A61K31/336 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/495 , A61P25/04 , A61P25/20 , A61P29/00 , C07C13/547 , C07C249/04 , C07C251/58 , C07C269/02 , C07C271/60 , C07D209/48 , C07D213/74 , C07D239/24 , C07D239/34 , C07D241/04 , C07D295/08 , C07D295/088 , C07D303/12 , C07D401/02 , C07D401/04 , C07C251/54
CPC分类号： C07D209/48 , C07C251/58 , C07C271/60 , C07D213/74 , C07D239/34 , C07D295/088 , C07D303/12 , C07C2101/02 , C07C2101/14 , C07C2103/16
摘要： The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; orA represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, whereinR.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; andR denotes hydrogen or C.sub.1-7 alkyl,stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.
摘要翻译：本发明涉及新的药学活性苯并[e]茚衍生物，其制备方法，包含其的药物组合物，进一步使用所述苯并[e]茚衍生物在某些疾病的治疗中以及在制备适于治疗所述疾病的药物组合物。根据本发明的新的苯并[e]茚衍生物对应于通式（I）其中A表示式alk-NR1R2的基团，其中alk表示任选携带羟基取代基的C 2-7亚烷基， R1和R2独立地是氢，C1-7烷基，C2-7烯基，C2-7炔基，单（C1-7）烷基氨基（C1-7）烷基，二（C1-7）烷基氨基（C1-7）烷基或 C3-7环烷基; 或R 1和R 2与它们所连接的氮原子一起形成4至7元环，任选地包含氧原子或另外的氮原子，后者可以携带苯基，苄基，吡啶基，嘧啶基或C 1-3烷基取代基，其取代基又可以具有羟基或甲氧基或卤素原子或卤代苯基; 或R 1和R 2与它们所连接的氮原子一起形成苯二甲酰亚氨基; 或A表示嘧啶基，2,3-环氧丙基或式-C（O）NHR 3的基团，其中R 3表示C 1-7烷基，C 2-7烯基或C 3-8环烷基; R表示氢或C 1-7烷基，立体异构体和旋光异构体及其可能的混合物，这些化合物的其它酸加成盐和季铵衍生物。

23. 发明授权

US5597822A Pharmaceutical compositions for the prevention and/or treatment a gastrointestinal diseases 失效
标题翻译：用于预防和/或治疗胃肠道疾病的药物组合物
公开(公告)号：US5597822A
公开(公告)日：1997-01-28
申请号：US443487
申请日：1995-05-18
申请人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
发明人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
IPC分类号： A61K31/15 , A61K31/495 , A61K31/50 , A61K31/505
CPC分类号： A61K31/15 , A61K31/495
摘要： The invention refers to pharmaceutical compositions for the prevention and/or treatment of gastrointestinal diseases connected with infections caused by Helicobacter pylori and a method for the treatment of such diseases.The pharmaceutical composition of the invention comprises as active ingredient a cyclic ketone derivative of the formula I ##STR1## wherein and R.sup.1 mean independently hydrogen or halo;R.sup.0 stands for hydrogen or a C.sub.1-4 alkoxy group;R.sup.2 and R.sup.3 independently represent hydrogen; a straight or branched chain C.sub.1-8 alkyl optionally substituted by a dimethylamino group; a C.sub.2-6 alkenyl or a C.sub.3-7 cycloalkyl group; orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 6-membered heterocyclic group containing an additional nitrogen atom that may bear a phenyl group optionally substituted by a C.sub.1-4 alkoxy group;or its stereoisomer or optical isomer or a possible mixture thereof, or a pharmaceutically acceptable acid addition salt or quaternary ammonium salt thereof in admixture with carrier(s) commonly used in pharmaceutical compositions.
摘要翻译：本发明涉及用于预防和/或治疗与由幽门螺杆菌引起的感染有关的胃肠道疾病的药物组合物和治疗这些疾病的方法。本发明的药物组合物包含作为活性成分的式I（I）的环酮衍生物，其中R 1独立地表示氢或卤素; R0表示氢或C1-4烷氧基; R2和R3独立地表示氢; 任选被二甲基氨基取代的直链或支链C 1-8烷基; C 2-6烯基或C 3-7环烷基; 或者R 2和R 3与相邻的氮原子一起形成含有另外的氮原子的6元杂环基，其可以具有任选被C 1-4烷氧基取代的苯基; 或其立体异构体或光学异构体或其可能的混合物，或其药学上可接受的酸加成盐或季铵盐与药物组合物中通常使用的载体混合。

24. 发明授权

US5942506A 1-�2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives 失效
标题翻译： 1- [2-（取代的乙烯基）] - 5H-2,3-苯并二氮杂衍生物
公开(公告)号：US5942506A
公开(公告)日：1999-08-24
申请号：US599236
申请日：1996-02-09
申请人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Istvan Gacsalyi , Andras Bilkei-Gorzo , Andras Egyed , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Hilda Botka , Tamas Hamori , Cecilia Salamon Haskane , Edit Horvath , Katalin Horvath , Peter Korosi , Gyorgyne Mate , Imre Moravcsik , Eszter Szentkuti , Gabor Zolyomi , Gabor Blasko , Klara Daroczi Kazone , Gyula Simig , Karoly Tihanyi , Judit Bajnogel
发明人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Istvan Gacsalyi , Andras Bilkei-Gorzo , Andras Egyed , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Hilda Botka , Tamas Hamori , Cecilia Salamon Haskane , Edit Horvath , Katalin Horvath , Peter Korosi , Gyorgyne Mate , Imre Moravcsik , Eszter Szentkuti , Gabor Zolyomi , Gabor Blasko , Klara Daroczi Kazone , Gyula Simig , Karoly Tihanyi , Judit Bajnogel
IPC分类号： A61K31/55 , A61K31/551 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , C07D243/02 , C07D243/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D491/04 , C07D491/056 , C07D493/04
CPC分类号： C07D405/06 , C07D243/02 , C07D491/04 , C07D493/04
摘要： This invention relates to new 1-�2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said benzodiazepine derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The compounds according to the invention correspond to the general formula (I), ##STR1## wherein the variables are herein below defined, and the compounds possess central nervous activities.
摘要翻译：本发明涉及新的1- [2-（取代的乙烯基）] - 5H-2,3-苯并二氮杂衍生物，其制备方法，包含其的药物组合物，涉及使用所述苯并二氮杂衍生物治疗疾病和用于制备适于治疗疾病的药物组合物。根据本发明的化合物对应于通式（I），其中变量在本文下面定义，并且化合物具有中枢神经活性。

25. 发明申请

US20080021016A1 Combined Pharmaceutical Composition for the Inhibition of the Decline of Cognitive Functions 审中-公开
标题翻译：用于抑制认知功能下降的组合药物组合物
公开(公告)号：US20080021016A1
公开(公告)日：2008-01-24
申请号：US10592461
申请日：2004-03-12
申请人： Gyorgy Levay , Istvan Gacsalyi , Laszlo Harsing , Gyula Simig
发明人： Gyorgy Levay , Istvan Gacsalyi , Laszlo Harsing , Gyula Simig
IPC分类号： A61K31/135 , A61K31/13 , A61K31/4015 , A61K31/437 , A61K31/55 , A61P25/28
CPC分类号： A61K45/06 , A61K31/135 , A61K31/355 , A61K31/4015 , A61K31/445 , A61K31/475 , A61K31/55 , A61K2300/00
摘要： The invention relates to a combined pharmaceutical composition for the inhibition of the decline of cognitive functions comprising as A) component (1R,2S,4R)-(-)-2-[N,N-(dimethylaminoethoxy)]-2-phenyl-1,7,7-trimethylbicyclo]-2-phenyl-1.7.-trimethylbicyclo[2.2.1]heptane of the formula (I) or a pharmaceutically acceptable acid addition salt thereof and as B) component a nootropic, an inhibitor of the acetylcholinesterase enzyme and/or a further pharmaceutical active ingredient which exhibits a beneficial effect on the cognitive processes in admixture with suitable inert pharmaceutical carriers and/or auxiliary agents. The combined pharmaceutical composition according to the present invention can be particularly used for the treatment of Alzheimer disease or other diseases showing similar symptoms, diseases accompanied by malfunctions of intellectual abilities (e.g. mental decline in schizophrenia), mental decline in elderly (dementias in elderly), Korsakoff syndrome, Huntington syndrome, Parkinson syndrome or mental decline produced by alcoholism.
摘要翻译：本发明涉及用于抑制认知功能下降的组合药物组合物，其包含A）成分（1R，2S，4R） - （ - ） - 2- [N，N-（二甲基氨基乙氧基）] -2-苯基 - （I）的1,7,7-三甲基双环] -2-苯基-1,7-三甲基双环[2.2.1]庚烷或其药学上可接受的酸加成盐和作为B）组分的向异性，乙酰胆碱酯酶的抑制剂酶和/或另外的药物活性成分，其与合适的惰性药物载体和/或辅助剂混合显示对认知过程的有益作用。根据本发明的组合药物组合物可以特别用于治疗阿尔茨海默氏病或类似症状的其他疾病，伴有智力障碍的疾病（例如精神分裂症的精神下降），老年人精神衰退（老年痴呆症），Korsakoff综合征，亨廷顿综合症，帕金森综合征或酒精中毒引起的精神衰弱。

26. 发明授权

US5716986A Oxaindene derivatives and process for the preparation thereof 失效
标题翻译：氧化烯衍生物及其制备方法
公开(公告)号：US5716986A
公开(公告)日：1998-02-10
申请号：US671515
申请日：1996-06-27
申请人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
发明人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
IPC分类号： C07D307/79 , A61K31/34 , A61K31/343 , A61K31/445 , A61K31/535 , A61P1/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D307/91 , C07D307/93
CPC分类号： C07D307/91 , C07D307/93
摘要： This invention relates to new oxaindene derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The compounds according to the invention are characterized by the general formula (1) ##STR1## wherein R.sup.1 represents lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or lower C.sub.3-6 cycloalkyl, R.sup.2 stands for hydrogen, lower C.sub.1-4 alkyl or lower C.sub.3-6 cycloalkyl, R.sup.3 stands for hydrogen, lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or benzyloxy, X denotes hydrogen, an aliphatic C.sub.1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C.sub.1-4 -alkoxy group(s) or a group of the formula R.sup.5 R.sup.6 N--R.sup.7 --, wherein R.sup.7 represents lower C.sub.1-4 alkylene and R.sup.5 and R.sup.6 each represent lower C.sub.1-4 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group, A and B together form an ethylene or a vinylene group, and n is 1, 2 or 3, and have a strong 5-lipoxygenase (5-LO) enzyme inhibiting activity.
摘要翻译：本发明涉及新的氧杂茚衍生物，其制备方法和包含其的药物组合物。根据本发明的化合物的特征在于通式（1）其中R 1表示低级C 1-4烷基，低级C 1-4烷氧基或低级C 3-6环烷基，R 2表示氢，低级C 1〜 4烷基或低级C3-6环烷基，R3代表氢，低级C1-4烷基，低级C1-4烷氧基或苄氧基，X表示氢，脂族C1-4酰基或苯甲酰基或萘甲酰基，任选被1或更多的硝基或C 1-4 - 烷氧基或式R 5 R 6 N-R 7 - 的基团，其中R 7表示低级C 1-4亚烷基，R 5和R 6各自表示低级C 1-4烷基，或者R 5和R 6连同它们所连接的氮原子形成哌啶基或吗啉基，A和B一起形成乙烯或亚乙烯基，n为1,2或3，具有强的5-脂氧合酶（5-LO）酶抑制活性。

27. 发明授权

US5523303A Trisubstituted cycloalkane derivatives and process for the preparation thereof 失效
标题翻译：三取代环烷烃衍生物及其制备方法
公开(公告)号：US5523303A
公开(公告)日：1996-06-04
申请号：US226051
申请日：1994-04-11
申请人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
发明人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P1/04 , C07C249/12 , C07C251/58 , C07D295/08 , C07D295/088 , C07D317/58
CPC分类号： C07D295/088 , C07C251/58 , C07C2101/08 , C07C2101/14 , C07C2101/18 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.1-4 alkoxy, or together represent a 3,4-methylenedioxy group,n is an integer from 2 to 5,A represents a valency bond or a --CH.sub.2 -- group.The compounds exert a valuable antiulcer effect, so they can be used to advantage in the therapy.
摘要翻译：本发明涉及新颖的药学活性三取代环烷烃衍生物，其制备方法和包含其的药物组合物。本发明还包括所述环烷烃衍生物用于治疗疾病和制备适于治疗疾病的药物组合物的用途。根据本发明的化合物的特征在于通式（I），其中R表示氢，C 1-4烷基或羟基，R 1表示C 1-12烷基，R 2和R 3各自表示氢，C 1 -12烷基或C2-12烯基，或R2和R3与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4-至7-元环，后者可以携带苯基，苄基或C1 -4-烷基取代基，R4和R5各自代表氢，卤素或C1-4烷氧基，或一起代表3,4-亚甲二氧基，n是2至5的整数，A表示价键或-CH 2 - 组。这些化合物具有有价值的抗溃疡作用，因此可用于治疗。

28. 发明申请

US20120116082A1 PROCESS FOR THE PREPARATION OF ROSUVASTATIN SALTS 失效
标题翻译：制备罗司他汀盐的方法
公开(公告)号：US20120116082A1
公开(公告)日：2012-05-10
申请号：US13143943
申请日：2010-01-15
申请人： Gyoergyi Kovanyin Lax , Eva Sipos , Jozsef Barkoczy , Balazs Volk , Gyula Simig , Ferenc Bartha , Gyoergy Ruzsics , Adrienn Karasz , Imre Kiraly , Kalman Nagy
发明人： Gyoergyi Kovanyin Lax , Eva Sipos , Jozsef Barkoczy , Balazs Volk , Gyula Simig , Ferenc Bartha , Gyoergy Ruzsics , Adrienn Karasz , Imre Kiraly , Kalman Nagy
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to a new process for the preparation of rosuvastatin [7-[4-(4-Fluorophenyl)-6-isopropyl-2-(methanesulphonyl-methyl-amino)-pyrimidin-5-yl]-(3R,51S)-dihydroxy-hept-6-enoic acid] of the formula (I) salts formed with bivalent cations, preferably with calcium or zinc ions, characterized in that rosuvastatin tert.-butylammonium salt is reacted with the appropriate bivalent cation, preferably with calcium or zinc ions in a mixture of a water immiscible or slightly miscible organic solvent and water and the formed salt is isolated.
摘要翻译：本发明涉及一种制备瑞舒伐他汀[7- [4-（4-氟苯基）-6-异丙基-2-（甲磺酰基 - 甲基 - 氨基） - 嘧啶-5-基] - （3R，51S ） - 二羟基 - 庚-6-烯酸]与二价阳离子形成的盐，优选与钙或锌离子形成，其特征在于，瑞舒伐他汀叔丁基铵盐与适当的二价阳离子，优选与钙或与水不混溶或与水混溶的有机溶剂和水的混合物中的锌离子与形成的盐分离。

29. 发明申请

US20130338360A1 METHOD FOR THE PREPARATION OF HIGH-PURITY PHARMACEUTICAL INTERMEDIATES 有权
标题翻译：制备高纯度药物中间体的方法
公开(公告)号：US20130338360A1
公开(公告)日：2013-12-19
申请号：US13990283
申请日：2011-11-29
申请人： Gyorgyi Kovanyine Lax , Gyula Simig , Balazs Volk , Ferenc Lorant Bartha , Gyorgy Krasznai , Gyorgy Ruzsics , Eva Sipos , Kalman Nagy , Gyorgy Morovjan , Jozsef Barkoczy , Adrienn Keszthelyi , Janos Imre , Gabor Bagyinszki
发明人： Gyorgyi Kovanyine Lax , Gyula Simig , Balazs Volk , Ferenc Lorant Bartha , Gyorgy Krasznai , Gyorgy Ruzsics , Eva Sipos , Kalman Nagy , Gyorgy Morovjan , Jozsef Barkoczy , Adrienn Keszthelyi , Janos Imre , Gabor Bagyinszki
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , A61K31/505
摘要： The present invention is related to intermediates useful in the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid and polymorphs of said intermediates, methods for preparation thereof and use thereof.
摘要翻译：本发明涉及可用于制备（+） - 7- [4-（4-氟苯基）-6-异丙基-2-（甲磺酰基 - 甲基 - 氨基） - 嘧啶-5-基的药用盐的中间体 ] - （3R，5S） - 二羟基 - 庚-6-烯酸和所述中间体的多晶型物，其制备方法和用途。

30. 发明授权

US09260421B2 Pharmaceutical intermediates and process for the preparation thereof 有权
标题翻译：药物中间体及其制备方法
公开(公告)号：US09260421B2
公开(公告)日：2016-02-16
申请号：US14116464
申请日：2012-05-10
申请人： Imre Kiraly , Tibor Szabo , Gyula Simig , Balazs Volk , Laszlo Szlavik , Jozsef Barkoczy , Gyorgy Ruzsics , Gyula Lukacs , Laszlo Pongo , Andras Boza , Maria Tothne Lauritz , Maria Kovacs
发明人： Imre Kiraly , Tibor Szabo , Gyula Simig , Balazs Volk , Laszlo Szlavik , Jozsef Barkoczy , Gyorgy Ruzsics , Gyula Lukacs , Laszlo Pongo , Andras Boza , Maria Tothne Lauritz , Maria Kovacs
IPC分类号： C07D271/06 , C07D413/14 , C07D401/12
CPC分类号： C07D413/14 , C07D271/06 , C07D401/12
摘要： The present invention relates to a process for the preparation of dabigatran etexilate of the formula or pharmaceutically accepted salts thereof.
摘要翻译：本发明涉及制备下式的达比加群酯或其药学上可接受的盐的方法。

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