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1. 发明申请

WO2007039781A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007039781A2
公开(公告)日：2007-04-12
申请号：PCT/HU2006/000087
申请日：2006-10-05
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , GÁL, Krisztina , WÉBER, Csaba , WÁGNER, Gábor, András , HORVÁTH, Attila , NYÉKI, Györgyné , VASTAG, Mónika , KESERÜ, György
发明人： GÁL, Krisztina , WÉBER, Csaba , WÁGNER, Gábor, András , HORVÁTH, Attila , NYÉKI, Györgyné , VASTAG, Mónika , KESERÜ, György
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4245 , A61P25/00
CPC分类号： C07D417/14 , C07D413/04 , C07D413/12
摘要： The present invention relates to new compounds of formula (I) wherein Y 1 and Y 2 selected from the group consisting of hydrogen, halogen atom; C 1-4 alkyl, C 1-4 alkoxy, cyano and trifluoromethyl group, Q is -CH- group or N; X 1 and X 2 are different and are independently selected from N and O; Z is -(CH 2 )n- group or S; n is 1 or 2; R is selected from the group consisting of optionally substituted C 1-7 alkyl, C 1-4 haloalkyl, C 1-4 hydroxyalkyl, C 1-4 cyanoalkyl, C 1-3 OC 1-3 alkyl, C 2-7 alkenyl, C 2-7 alkynyl, C 0-2 (NR 1 R 2 )alkyl; an optionally substituted C 3-7 cycloalkyl, aryl, heteroaryl or saturated heterocyclyl; R 1 and R 2 are independently selected from hydrogen, C 1-7 alkyl or C 1-6 alkanoyl group - and/or enentiomers and/or racemates and/or diastereomers and/or geometric isomers and/or pharmaceutically acceptable salts thereof formed with acids and bases, to the processes for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：本发明涉及新的式（I）化合物，其中Y 1和Y 2选自氢，卤素原子， C 1-4烷基，C 1-4烷氧基，氰基和三氟甲基，Q是-CH-基或N; X 1和X 2不同，并且独立地选自N和O; Z是 - （CH 2 CH 2）n - 基或S; n为1或2; R选自任选取代的C 1-7 - 烷基，C 1-4 - 卤代烷基，C 1-4 - 1-4羟基烷基，C 1-4个碳原子的烷基，C 2-7链烯基，C C 2-7炔基，C 0-2 - （NR 1 R 2）2 - 烷基; 任选取代的C 3-7环烷基，芳基，杂芳基或饱和杂环基; R 1和R 2独立地选自氢，C 1-7 - 烷基或C 1-6 - 烷酰基与酸和碱形成的基团和/或环戊二烯基和/或异构体和/或非对映异构体和/或其几何异构体和/或其药学上可接受的盐，涉及制备所述化合物的方法，含有所述化合物的药物组合物及其用途在预防和/或治疗mGluR5受体介导的疾病中。

2. 发明申请

WO2007072093A1 QUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF MGLUR5 RECEPTOR-MEDIATED DISORDERS 审中-公开
标题翻译：喹诺酮衍生物用于治疗MGLUR5受体介导的疾病
公开(公告)号：WO2007072093A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000121
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , KESERÜ, György , WÉBER, Csaba , BIELIK, Attila , BOBOK, Amrita, Ágnes , GÁL, Krisztina , MESZLÉNYINÉ SIPOS, Márta , MOLNÁR, László , VASTAG, Mónika
发明人： KESERÜ, György , WÉBER, Csaba , BIELIK, Attila , BOBOK, Amrita, Ágnes , GÁL, Krisztina , MESZLÉNYINÉ SIPOS, Márta , MOLNÁR, László , VASTAG, Mónika
IPC分类号： A61K31/4706 , A61K31/4709 , A61K31/4741 , C07D215/42 , C07D215/44 , C07D215/46 , C07D401/04 , C07D405/12 , C07D405/14 , A61P25/00
CPC分类号： C07D215/42 , C07D215/44 , C07D215/46 , C07D405/12 , C07D491/04 , C07D491/10
摘要： Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation, to the intermediates of the preparation process, to the pharmaceutical formulations containing these compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：与酸或碱形成的式（I）化合物和/或其对映异构体和/或外消旋体和/或非对映异构体和/或其药学上可接受的盐，其制备方法，制备方法的中间体，含有这些化合物的制剂及其在预防和/或治疗mGluR5受体介导的病症中的用途。

3. 发明申请

WO2007072092A2 NEW PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS 审中-公开
标题翻译：新的苯丙氨酸衍生物作为布拉霉素拮抗剂
公开(公告)号：WO2007072092A2
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000120
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BEKE, Gyula , BOZÓ, Éva , CZÍRA, Gábor , ÉLES, János , FARKAS, Sándor , HORNOK, Katalin , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
发明人： BEKE, Gyula , BOZÓ, Éva , CZÍRA, Gábor , ÉLES, János , FARKAS, Sándor , HORNOK, Katalin , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
IPC分类号： C07D213/74 , C07D221/12 , C07D295/12 , C07D401/10 , C07D401/12 , C07D401/14 , A61K31/473 , A61P25/02
CPC分类号： C07D401/12 , C07D213/74 , C07D221/12 , C07D295/135 , C07D401/10 , C07D401/14
摘要： The present invention relates to new phenanthridine derivatives of formula (I) wherein R 1 is hydrogen atom or C 1 -C 4 alkyl group; R 2 is selected from (1) hydrogen atom; with the proviso that R 1 and R 2 can not be simultaneously hydrogen atom; (2) -(CH 2 ) n -NR a R b , (3) -(CH 2 ) n -CO-NR a R b , (4) - (CH 2)m X-Q, (5) -CHR c -NR a R b ; or R 1 and R 2 together with the nitrogen atom to which they are attached form a 4-7 membered heterocyclic ring containing 1-3 heteroatom selected from O, S and N; wherein said ring is optionally substituted with -CO-NR a R b , C 1 -C 4 alkyl, 4-(4,5-dihydro-lH- imidazol-2-yl)-benzyl or 4-(l,4,5,6-tetrahydro-pyrimidin-2-yl)-benzyl; R 3 , R 4 , R 5 , R 6 and R 7 are independently of each other hydrogen atom, halogen atom, trifluoromethyl, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or acetyl group; n is an integer from 1 to 4; R a and R b are hydrogen atom, optionally substituted C 1 -C 4 alkyl group, or R a , R b and the nitrogen atom to which they are both attached together form a saturated, partially unsaturated or aromatic 4-7 membered ring containing 1-3 heteroatom selected from O, S and N; wherein said ring is optionally substituted with 1-piperidinyl, 2- piperidinyl, 4-piperidinyl, 2-pyridyl or 4-pyridyl group; R c is methyl, hydroxymethyl, benzyl or phenyl group; m is an integer from 0 to 6; X is a single bond, O or S; Q is a phenyl group, optionally substituted with [l,4']biρiperidinyl-l'-yl, 4,5-dihydro- lH-imidazol-2-yl, -(CH 2 )n-NH-(C=NH)-NH 2 or -(CH 2 )m-(C=NH)-NH 2 group; or 4- piperidinyl group, optionally substituted with 4-piperidinyl group; or C 5 -C 7 cycloalkyl group, optionally substituted with -(CH 2 ) m -NR a R b group, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.
摘要翻译：本发明涉及式（I）的新的菲啶衍生物，其中R 1是氢原子或C 1 -C 4烷基; R 2选自（1）氢原子; 条件是R 1和R 2不能同时为氢原子; （2） - （CH 2）n - ， - （CH 3） - （CH 2）（4） - （CH 2）m（CH 2）n - （CH 2）n - XQ，（5）-CHR 或R 1和R 2与它们所连接的氮原子一起形成含有1-3个选自O，S和N的杂原子的4-7元杂环 ; 其中所述环任选被-CO-NR a，C 1 -C 4烷基，C 1 -C 4烷基， 4-（4,5-二氢-1H-咪唑-2-基） - 苄基或4-（1,4,5,6-四氢 - 嘧啶-2-基） - 苄基; R 3，R 4，R 5，R 6和R 7均为独立于氢原子，卤素原子，三氟甲基，C 1 -C 4烷基，C 1 -C 4烷基，烷氧基或乙酰基; n是1至4的整数; R a和R b都是氢原子，任选取代的C 1 -C 4烷基，或者R 1，它们都连接在一起的氮原子形成饱和的，部分不饱和的或芳族的4-7元环，其含有1-3个选自O， S和N; 其中所述环任选被1-哌啶基，2-哌啶基，4-哌啶基，2-吡啶基或4-吡啶基取代; R c是甲基，羟甲基，苄基或苯基; m为0〜6的整数; X为单键，O或S; Q是任选被[1,4']二哌啶基-1'-基，4,5-二氢-1H-咪唑-2-基， - （CH 2）2 - 基取代的苯基， n-NH-（C = NH）-NH 2或 - （CH 2）2 - （C = NH）-NH 2基团 ; 或4-哌啶基，任选被4-哌啶基取代; 或C 5 -C 7环烷基，任选被 - （CH 2 CH 2）m -NR n O取代 >光学对映体或其外消旋体和/或其盐和/或其水合物和/或溶剂合物，其制备方法涉及含有该组合物的药物组合物并用于治疗或预防疼痛和炎症过程。

4. 发明申请

WO2008155588A1 SULFONYL-QUINOLINE DERIVATIVES 审中-公开
标题翻译：磺酰喹啉衍生物
公开(公告)号：WO2008155588A1
公开(公告)日：2008-12-24
申请号：PCT/HU2008/000068
申请日：2008-06-17
申请人： RICHTER GEDEON NYRT. , VASTAG, Mónika , GALAMBOS, János , KESERÛ, György , GÁL, Krisztina , BOBOK, Amrita, Ágnes , WÉBER, Csaba , PRAUDA, lnolya , WÁGNER, Gábor, András
发明人： GALAMBOS, János , KESERÛ, György , GÁL, Krisztina , BOBOK, Amrita, Ágnes , WÉBER, Csaba , PRAUDA, lnolya , WÁGNER, Gábor, András
IPC分类号： C07D215/36 , C07D409/12 , A61K31/4706 , A61K31/4709 , A61P25/00
CPC分类号： C07D215/36 , C07D409/12
摘要： New mGluRl and mGluR5 receptor subtype preferring ligands of formula: (I) and/or salts and/or hydrates and/or solvates thereof, to the processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in therapy and/or prevention of a condition which requires modulation of mGluRl and mGluR5 receptors.FORMULE (I) wherein Ar 1 represents an optionally substituted phenyl or heteroaryl group; Ar 2 represents a substituted phenyl or an optionally substituted heteroaryl group; R 1 , R 2 , R 3 and R 4 represent independently a substituent selected from hydrogen, halogen, cyano, alkyl, alkoxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl
摘要翻译：新的mGluR1和mGluR5受体亚型优选式（I）的配体和/或其盐和/或水合物和/或溶剂化物，其制备方法和中间体，含有这些化合物的药物组合物及其在治疗和 /或预防需要调节mGluR1和mGluR5受体的病症。其中Ar 1表示任选取代的苯基或杂芳基; Ar 2表示取代的苯基或任选取代的杂芳基; R1，R2，R3和R4独立地表示选自氢，卤素，氰基，烷基，烷氧基，羟基，三氟甲基，氨基，烷基氨基，二烷基氨基，氨基甲基，烷基氨基甲基，二烷基氨基甲基

5. 发明申请

WO2009053763A1 NEW NON-PEPTIDE DERIVATIVES AS BRADYKININ BL ANTAGONISTS 审中-公开
标题翻译：新的非肽衍生物作为BRADYKININ BL拮抗剂
公开(公告)号：WO2009053763A1
公开(公告)日：2009-04-30
申请号：PCT/HU2007/000101
申请日：2007-10-27
申请人： RICHTER GEDEON NYRT. , VÁGÓ, István , FARKAS, Sándor , HORNOK, Katalin , BEKE, Gyula , BOZÓ, Éva , VASTAG, Mónika , SZENTIRMAY, Éva , KESERÜ, György , SCHMIDT, Éva
发明人： VÁGÓ, István , FARKAS, Sándor , HORNOK, Katalin , BEKE, Gyula , BOZÓ, Éva , VASTAG, Mónika , SZENTIRMAY, Éva , KESERÜ, György , SCHMIDT, Éva
IPC分类号： C07C311/21 , A61K31/18 , A61P29/00 , C07D207/12 , C07D211/22 , C07D211/26 , C07D211/44 , C07D211/58 , C07D211/62 , C07D241/06 , C07D243/08 , C07D279/12 , C07D295/20 , C07D401/04
CPC分类号： C07C311/21 , C07D207/36 , C07D211/22 , C07D211/26 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/74 , C07D241/08 , C07D295/096 , C07D295/185
摘要： The present invention relates to new non-peptide derivatives of formula (I), wherein R 1 -R 5 , Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及式（I）的新的非肽衍生物，其中R 1 -R 5，Q和Z如权利要求中所定义，和光学对映体或外消旋体和/或其盐和/或其水合物和/或溶剂合物，其是缓激肽B1的选择性拮抗剂，用于制备这些化合物的方法，含有它们的药理学组合物及其在治疗或预防疼痛和炎症病症中的用途。

6. 发明申请

WO2008068540A1 NEW BENZAMIDE DERIVATIVES AS BRAD YKININ ANTAGONISTS 审中-公开
标题翻译：新的苯甲酸衍生物作为亚丁宁拮抗剂
公开(公告)号：WO2008068540A1
公开(公告)日：2008-06-12
申请号：PCT/HU2007/000102
申请日：2007-10-27
申请人： RICHTER GEDEON NYRT. , VÁGÓ, István , BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VASTAG, Mónika
发明人： VÁGÓ, István , BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VASTAG, Mónika
IPC分类号： C07D207/08 , A61K31/18 , A61P29/00 , C07D207/26 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/58 , C07D211/62 , C07D211/68 , C07D211/76 , C07D219/06
CPC分类号： C07D295/185 , C07D207/08 , C07D207/26 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/58 , C07D211/62 , C07D211/68 , C07D211/76 , C07D219/06 , C07D223/10 , C07D239/42 , C07D241/06 , C07D241/20 , C07D243/08 , C07D279/12 , C07D295/20 , C07D295/26 , C07D307/14 , C07D307/24 , C07D307/68 , C07D401/06 , C07D487/08
摘要： The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I), wherein R 1 -R 5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及式（I）的新的苯基氨磺酰基苯甲酰胺衍生物，其中R 1至Z 5和Z如权利要求中所定义，和光学对映体或外消旋体和作为缓激肽B1的选择性拮抗剂的盐和/或其水合物和/或溶剂合物，用于制备这些化合物的方法，含有它们的药物组合物及其在治疗或预防疼痛和炎症病症中的用途。

7. 发明申请

WO2008050167A1 NEW PHENYLSULFAMOYL BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS 审中-公开
标题翻译：新型苯甲酰苯胺衍生物作为布拉霉素拮抗剂
公开(公告)号：WO2008050167A1
公开(公告)日：2008-05-02
申请号：PCT/HU2007/000103
申请日：2007-10-27
申请人： RICHTER GEDEON NYRT. , BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
发明人： BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
IPC分类号： C07C311/21 , A61K31/18 , A61P29/00 , C07D209/08 , C07D211/26 , C07D211/58 , C07D213/40 , C07D231/40 , C07D233/54 , C07D235/30 , C07D261/14 , C07D277/46 , C07D277/62 , C07D277/82 , C07D285/12
CPC分类号： C07C311/21 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D211/26 , C07D211/58 , C07D213/40 , C07D213/75 , C07D231/40 , C07D233/54 , C07D233/64 , C07D235/30 , C07D241/08 , C07D261/14 , C07D277/46 , C07D277/62 , C07D277/82 , C07D285/135 , C07D295/13 , C07D295/135 , C07D317/46
摘要： The present invention relates to new sulfonamide derivatives of formula (I), wherein R 1 -R 8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及新的式（I）磺酰胺衍生物，其中R 1 -R 8和Z如权利要求中所定义，光学对映体或外消旋体和/ 或它们作为缓激肽B1的选择性拮抗剂的盐和/或水合物和/或溶剂合物，用于制备这些相同化合物的方法，含有它们的药物组合物及其在治疗或预防疼痛和炎症病症中的用途。

8. 发明申请

WO2007072094A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007072094A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000122
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
发明人： NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
IPC分类号： C07D495/04 , A61K31/4365 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from CO, SO, SO 2 ; Y represents a group selected from 0, OCH 2 , (CH 2 )n, NH, NHCH 2 ; n is an integer of 0 to 2; R 1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R 2 is an optionally substituted phenyl, heterocyclyl or NR 3 R 4 group wherein R 3 and R 4 are independently selected from the group of hydrogen, alkyl, or R 3 and R 4 together with the N atom to which they are attached can form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s) selected from the group of N, O, S, and/or tautomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自CO，SO，SO 2的基团; Y表示选自0，OCH 2，（CH 2）2，NH，NHCH 2的基团。 n为0〜2的整数， R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4 R 4基团，其中R 3'和R“_{> 4个独立地选自氢，烷基或R 3和R 4和它们所连接的N原子的基团可以形成含有一个或多个选自N，O，S和/或互变异构体和/或盐和/或水合物的杂原子和/或杂原子的任选取代的C 5-7杂环基，和/或其制备方法涉及含有该组合物的药物组合物及其在治疗和/或预防需要调节mGluR1和mGluR5受体如神经系统疾病，精神疾病，急性和慢性的病理状况中的用途疼痛，下尿路神经肌肉功能障碍和胃肠道疾病。}

9. 发明申请

WO2007072089A1 MGLUR5 ANTAGONISTIC CARBAMOYL-OXIME DERIVATIVES 审中-公开
标题翻译： MGLUR5拮抗性羰基氧化衍生物
公开(公告)号：WO2007072089A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000117
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETU GYÁR RT. , GALAMBOS, János , VASTAG, Mónika , BOBOK, Amrita, Ágnes , KESERÜ, György , GÁL, Krisztina , BENKÖ, Bernadett , RILL, Attila , DEMETER, Ádám
发明人： GALAMBOS, János , VASTAG, Mónika , BOBOK, Amrita, Ágnes , KESERÜ, György , GÁL, Krisztina , BENKÖ, Bernadett , RILL, Attila , DEMETER, Ádám
IPC分类号： C07C271/60 , C07D333/22 , C07D207/32 , C07D307/52 , C07D233/54 , C07D213/53 , C07D213/65 , C07D209/14 , C07D295/12 , C07D217/04 , A61K31/325 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/415
CPC分类号： C07C271/60 , C07C2601/14 , C07D207/335 , C07D209/14 , C07D213/53 , C07D213/65 , C07D217/02 , C07D233/54 , C07D233/61 , C07D295/135 , C07D307/52 , C07D333/22
摘要： The present invention relates to new mGluR5 receptor subtype preferring ligands of formula (I): (I) wherein R 1 and R 2 represent independently a substituent selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl and cyano; X is a CHR6 group or O; R 3 represents an alkyl substituent, R 4 and/or R 5 represent hydrogen, R 6 is hydrogen or alkyl, or R 3 and R 4 with the intermediate two carbon atoms together form a cyclohexane or cyclopentane ring and/or R 5 and R 6 together form a bond; Y is an optionally substituted phenyl or heterocyclyl, and/or enantiomers and/or racemates and/or diastereomers and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the process for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of niGluR5 receptor such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.
摘要翻译：本发明涉及式（I）的新型mGluR5受体亚型优选配体：（I）其中R 1和R 2独立地表示选自氢，卤素，烷基，烷氧基，卤代烷基和氰基; X是CHR6基团或O; R 3表示烷基取代基，R 4和/或R 5表示氢，R 6是氢或烷基或R 3和R 4与中间体两个碳原子一起形成环己烷或环戊烷环和/或R 5和R 5， SUB> 6 共同形成键; Y是任选取代的苯基或杂环基，和/或其对映异构体和/或外消旋体和/或非对映异构体和/或几何异构体和/或其盐和/或水合物和/或溶剂合物，含有其的组合物及其在治疗和/或预防需要调节niGluR5受体的病理状况的用途，例如神经系统疾病，精神病学障碍，急性和慢性疼痛以及下泌尿道的神经肌肉功能障碍。

10. 发明申请

WO2003082816A1 NEW ATORVASTATIN SALTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新的ATORVASTATIN SALTS和含有它们的药物组合物
公开(公告)号：WO2003082816A1
公开(公告)日：2003-10-09
申请号：PCT/HU2003/000024
申请日：2003-03-27
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , FISCHER, János , VUKICS, Krisztina , ERDÉLYI, Péter , HEGEDÜS, Béla , TIHANYI, Károly , VASTAG, Mónika , LÉVAI, Sándor , BÁLINT, Sándorné , LÁNCZOS, Krisztina
发明人： FISCHER, János , VUKICS, Krisztina , ERDÉLYI, Péter , HEGEDÜS, Béla , TIHANYI, Károly , VASTAG, Mónika , LÉVAI, Sándor , BÁLINT, Sándorné , LÁNCZOS, Krisztina
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： The invention relates to salts of atorvastatin formed with a basic amino acid of the general formula (I), where the meaning of R is a group originated from lysine, arginine or ornithine, and the amorphous or polymorph modifications thereof. The invention also relates to the synthesis of the compounds of the general formula (I).
摘要翻译：本发明涉及与通式（I）的碱性氨基酸形成的阿托伐他汀的盐，其中R的含义是衍生于赖氨酸，精氨酸或鸟氨酸的基团，以及其无定形或多晶型修饰。本发明还涉及通式（I）的化合物的合成。

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