专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1993001196A1 KETOALKYLGLYCEROPHOSPHOLIPIDS HAVING ANTITUMOR AND ANTI-PLATELET AGGREGATION ACTIVITIES, PROCESSES FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS THEREFROM 审中-公开
标题翻译：具有抗肿瘤剂和抗肿瘤活性的酮二磷酸胆固醇，其制备方法及其药物组合物
公开(公告)号：WO1993001196A1
公开(公告)日：1993-01-21
申请号：PCT/EP1992001502
申请日：1992-07-03
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , FOS TORRO, Maria de los Desemparados
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07F09/10
CPC分类号： C07F9/10 , C07F9/58 , C07F9/6506 , C07F9/6539
摘要： Compounds of general formula (I) wherein R is a C1-C16 straight or branched alkyl group, a phenyl group or a phenyl-C6-C16alkyl group; n is an integer from 3 to 18, inclusive; R is a C1-C12 straight or branched alkyl group; R is hydrogen, a carboxy, alkoxycarbonyl, arylalkoxycarbonyl or aryloxycarbonyl group of less than 12 carbon atoms in the last three cases; R , R and R , which can be the same or different, are hydrogen, a C1-C6 alkyl group or N R R R is a cyclic ammonium group, which can be aromatic or non-aromatic, wherein two of the R , R or R groups form a ring together with the nitrogen atom, and the other group is hydrogen or C1-C6 alkyl, have antitumor and anti-platelet aggregating activities.
摘要翻译：通式（I）的化合物，其中R 1是C 1 -C 16直链或支链烷基，苯基或苯基-C 6 -C 16烷基; n为3〜18的整数，包括3〜18的整数。 R 2是C 1 -C 12直链或支链烷基; 在最后三种情况下，R 3为氢，碳原子数为少于12个碳原子的羧基，烷氧基羰基，芳基烷氧基羰基或芳氧基羰基; R 4，R 5和R 6可以相同或不同，是氢，C 1 -C 6烷基或N + R 4 R 5 R 6是环状铵基，其可以是芳族或非芳族的，其中R 4，R 5或R 6中的两个与氮原子一起形成环，另一个基团是氢或C 1 -C6烷基，具有抗肿瘤和抗血小板聚集活性。

2. 发明申请

WO1994011332A1 A NOVEL ARYLPROPIONIC DERIVATIVE, A PROCESS FOR THE PREPARATION AND THE USE THEREOF AS AN ANALGESIC AGENT 审中-公开
标题翻译：新型芳基衍生物，其制备方法及其作为药物代谢物的用途
公开(公告)号：WO1994011332A1
公开(公告)日：1994-05-26
申请号：PCT/EP1993003127
申请日：1993-11-09
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , GARCIA PEREZ, M. Luisa
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07C59/84
CPC分类号： C07C215/10 , C07C59/84
摘要： A novel arylpropionic derivative, i.e. the (+)-(S)-2-(3-Benzoylphenyl)propionic acid tromethamine salt, the process for the preparation thereof and the use thereof as an analgesic and antiinflammatory agent.
摘要翻译：一种新的芳基丙酸衍生物，即（+） - （S）-2-（3-苯甲酰基苯基）丙酸氨丁三醇盐，其制备方法及其作为镇痛和抗炎剂的用途。

3. 发明申请

WO1996029325A1 HOMOCHIRAL COMPOUNDS FOR THE PREPARATION OF KETOCONAZOLE, TERCONAZOLE AND RELATED ANTIFUNGAL DRUGS 审中-公开
标题翻译：用于制备酮康唑，妥康唑和相关抗真菌药物的合成化合物
公开(公告)号：WO1996029325A1
公开(公告)日：1996-09-26
申请号：PCT/EP1996000972
申请日：1996-03-07
申请人： LABORATORIOS MENARINI S.A. , CAMPS GARCIA, Pelayo , FARRES TORRECABOTA, Xavier , MAULEON CASELLAS, David , CARGANICO, Germano , GARCIA PEREZ, Maria Luisa
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07D317/24
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D317/24
摘要： The present invention relates to novel homochiral compounds which are intermediates for the preparation of a number of azole antifungal drugs of formula (V), in an enantiomerically pure form, wherein Ar is a phenyl or substituted phenyl group, so that the substituted phenyl group can contain one to three substituents, which can independently be fluorine, chlorine, bromine, (C1-C4)-alkyl or (C1-C4)-alkyloxy; Y is a CH group or a nitrogen atom; Z is a group COCH3, CH(CH3)2 or (a). The present invention also relates to the compounds (+)-terconazole and (-)-terconazole. Said compounds show antifungal and antibacterial activities and they can be used in human and veterinary therapies.
摘要翻译：本发明涉及作为制备多种式（Ⅴ）的唑类抗真菌药物的对映体纯形式的中间体，其中Ar为苯基或取代的苯基，使得取代的苯基可以含有一至三个取代基，其可以独立地为氟，氯，溴，（C 1 -C 4） - 烷基或（C 1 -C 4） - 烷氧基; Y是CH基或氮原子; Z是COCH 3，CH（CH 3）2或（a）。本发明还涉及化合物（+） - 特康唑和（ - ） - 特康唑。所述化合物显示抗真菌和抗菌活性，并且它们可用于人和兽医疗法。

4. 发明申请

WO1996004246A1 PHENYLACETAMIDES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION 审中-公开
标题翻译：具有白藜芦醇拮抗作用的苯乙烯胺
公开(公告)号：WO1996004246A1
公开(公告)日：1996-02-15
申请号：PCT/EP1995002958
申请日：1995-07-26
申请人： LABORATORIOS MENARINI S.A. , MAULEON CASELLAS, David , CARGANICO, Germano , GARCIA PEREZ, Maria, Luisa , FOS TORRO, Mª de los Desamparados
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07D215/14
CPC分类号： C07D401/12 , C07D215/14 , C07D215/18
摘要： Phenylacetamides of formula (I) wherein the substituent containing a -CONR - is bound to the 3- or 4- position of the phenol system; the substituent containing B is bound to the benzene ring at any free position; R is hydrogen, fluorine, chlorine or -OCH3; R is hydrogen, fluorine, chlorine or bromine; R is hydrogen or methyl; B is a 5-tetrazolyl group or -COOR , wherein R is hydrogen, a (C1-C4)-alkyl or a phenylalkyl group of less than 10 carbon atoms; m and n are integers from 0 to 6, with the proviso that m + n is less or equal to 6; have leukotriene antagonistic action.
摘要翻译：式（I）的苯乙酰胺，其中含有-CONR 3的取代基与苯酚体系的3-或4-位结合; 含有B的取代基在任何自由位与苯环结合; R 1是氢，氟，氯或-OCH 3; R 2是氢，氟，氯或溴; R 3是氢或甲基; B是5-四唑基或-COOR 4，其中R 4是氢，少于10个碳原子的（C 1 -C 4） - 烷基或苯基烷基; m和n是0至6的整数，条件是m + n小于或等于6; 具有白三烯拮抗作用。

5. 发明申请

WO1993025703A1 A PROCESS FOR THE PREPARATION OF S-(+)-2-(3-BENZOYLPHENYL)PROPIONIC ACID BY ENZYME-CATALYSED ENANTIOSELECTIVE HYDROLYSIS 审中-公开
标题翻译：通过酶催化的选择性水解制备S - （+） - 2-（3-苯甲酰基）丙酸的方法
公开(公告)号：WO1993025703A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001321
申请日：1993-05-26
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , PALOMER BENET, Albert
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C12P41/00
CPC分类号： C12P41/005 , C12P7/40
摘要： A process for the preparation of optically active S-(+)-2-(3-benzoylphenyl)propionic acid (I), by resolution of the racemate through enantioselective hydrolysis of a reactive ester (II) in an organic medium, which hydrolysis is catalysed by an extracellular lipase of microbial origin. The separation of the resulting free acid from the remaining ester is carried out by extraction in basic medium, to leave the S-ester in the organic phase and the R-acid in the aqueous one. Finally, the desired S isomer is obtained either by aqueous hydrolysis of the remaining reactive S-ester, at constant pH, or enzymatically.
摘要翻译：通过在有机介质中反应性酯（II）的对映选择性水解来拆分外消旋物，制备光学活性的S - （+） - 2-（3-苯甲酰基苯基）丙酸（I）的方法，该水解为由微生物来源的细胞外脂肪酶催化。所得游离酸与剩余的酯的分离是通过在碱性介质中萃取进行的，以使有机相中的S-酯和含水的R酸。最后，所需的S异构体可以通过在恒定pH或酶促水解残留的活性S-酯获得。

6. 发明申请

WO1993025704A1 A PROCESS FOR THE PREPARATION OF S-(+)-2-(3-BENZOYLPHENYL)PROPIONIC ACID BY ENZYME-CATALYSED ENANTIOSELECTIVE TRANSESTERIFICATION IN AN ORGANIC SOLVENT 审中-公开
标题翻译：通过在有机溶剂中通过酶催化的选择性离子交换制备S - （+） - 2-（3-苯甲酰基）丙酸的方法
公开(公告)号：WO1993025704A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001322
申请日：1993-05-26
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , PALOMER BENET, Albert
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C12P41/00
CPC分类号： C12P41/005 , C12P7/62
摘要： A process for the preparation of S-(+)-2-(3-benzoylphenyl)propionic acid, according to formula (I), which process comprises the following steps: a) stereoselective transesterification in organic medium, catalysed by a carboxylesterase enzyme of microbial origin, of an ester of formula (II) in which R is a C1-C10 straight, branched or cyclic alkyl group, which can be substituted at the alpha - or beta -positions by an electron-withdrawing group, said transesterification reaction is carried out in an organic solvent with an alcohol of general formula R OH, R being a C1-C8 straight, branched or cyclic alkyl group, or a C1-C4 straight, branched or cyclic alkyl group substituted by a group having acid or basic functionality; b) selective hydrolysis or extraction of ester IV which is then converted to I.
摘要翻译：根据式（I）制备S - （+） - 2-（3-苯甲酰基苯基）丙酸的方法，该方法包括以下步骤：a）有机介质中的立体选择性酯交换反应，由羧酸酯酶催化微生物来源的式（II）的酯，其中R 1是可以被吸电子基团在α或β-位上取代的C 1 -C 10直链，支链或环状烷基，所述酯交换反应在有机溶剂中与通式为R 5 OH的醇进行，R 5为C 1 -C 8直链，支链或环状烷基或C 1 -C 4直链，支链或环状烷基被具有酸或碱官能团的基团取代; b）选择性水解或提取酯IV，然后将其转化为I.

7. 发明申请

WO1993021211A1 AMIDES HAVING INHIBITING ACTIVITY ON PHOSPHOLIPASE A2, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：具有磷脂酶A2抑制活性的氨基酸，其制备方法和含有它们的药物组合物
公开(公告)号：WO1993021211A1
公开(公告)日：1993-10-28
申请号：PCT/EP1993000866
申请日：1993-04-07
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , GARCIA PEREZ, Maria Luisa
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07K05/06
CPC分类号： C07K5/06069 , A61K38/00 , C07C323/60 , Y02P20/55
摘要： The present invention relates to amides of general formula (I), a process for the preparation thereof and pharmaceutical compositions containing them. In formula (I), X is oxygen or sulphur; R is alkyl; R is hydrogen, alkylcarbonyl, alkoxycarbonyl or alkylsulfonyl or the corresponding arylalkyl groups; R is hydrogen, carboxyl, alkoxycarbonyl or aryloxycarbonyl; and R hydrogen, alkyl, arylalkyl, heteroarylalkyl, hydroxyalkyl, thioalkyl, alkylthioalkyl, aminoalkyl, carboxyalkyl, carbamoyl, guanidinoalkyl or sulfoalkyl. Said compounds inhibit phospholipase A2, therefore they can be used as antiinflammatory, antiallergic, antithrombotic, antiasthmatic agents and in the prevention of anaphylactic shock. Said amides can be obtained by reacting a compound (II), wherein R is the same as R or a suitable protecting group, with a suitable amine H2NCHR R , in the presence of a proton-binding base and a carboxy-activating agent.
摘要翻译：本发明涉及通式（I）的酰胺，其制备方法和含有它们的药物组合物。在式（I）中，X是氧或硫; R 1是烷基; R 2是氢，烷基羰基，烷氧基羰基或烷基磺酰基或相应的芳基烷基; R 3是氢，羧基，烷氧基羰基或芳氧基羰基; 烷基，芳基烷基，杂芳基烷基，羟基烷基，硫代烷基，烷基硫代烷基，氨基烷基，羧基烷基，氨基甲酰基，胍基烷基或磺基烷基。所述化合物抑制磷脂酶A2，因此它们可以用作抗炎，抗过敏，抗血栓形成，止喘药和用于预防过敏性休克。所述酰胺可以通过使其中R 6与R 2相同的化合物（II）或合适的保护基与合适的胺H 2 NCHR 3 R 4在质子结合碱和羧基活化剂。

8. 发明申请

WO1997034885A1 BENZOPYRAN DERIVATIVES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION 审中-公开
标题翻译：具有白介素拮抗作用的苯并吡喃衍生物
公开(公告)号：WO1997034885A1
公开(公告)日：1997-09-25
申请号：PCT/EP1997001418
申请日：1997-03-20
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , PASCUAL AVELLANA, Jaime , GARCIA PEREZ, Mª Luisa , PALOMER BENET, Albert
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07D311/58
CPC分类号： C07D405/12 , C07C45/54 , C07C205/45 , C07D311/24 , C07D405/04 , Y02P20/55 , C07C49/825
摘要： The present invention relates to novel benzopyran derivatives of formula (I), wherein A is an oxygen or sulfur atom or a methylene group; B and C are: a) when B is a benzofused heterocycle (a) wherein U is an O, S or N atom, Z-Y are two carbon atoms linked by a double or single bond and T is a single bond, a methylene or carbonyl group, C can be a -CONR -, CSNR -, -SO2NR -, -CH2O-, -CH=CH- group; b) when B is a phenyl group (b), C can be a -SO2NR -, -CH2O-, -CH=CH- group; D is a 5-tetrazolyl or -COOR group, wherein R is hydrogen, a (C1-C4)-alkyl or phenylalkyl group; and m and n are integers between 0 and 4. Said compounds show a leukotriene-antagonistic activity, and they are valuable as anti-inflammatory and antiallergic medicaments or in the treatment of cardiovascular diseases.
摘要翻译：本发明涉及式（I）的新型苯并吡喃衍生物，其中A为氧或硫原子或亚甲基; B和C是：a）当B是苯并稠合的杂环（a）其中U是O，S或N原子时，ZY是通过双键或单键连接的两个碳原子，T是单键，亚甲基或羰基基团，C可以是-CONR 7 - ，CSNR 7 - ， - SO 2 NR 7 - ， - CH 2 O - ， - CH = CH-基团; b）当B是苯基（b）时，C可以是-SO 2 NR 7 - ， - CH 2 O - ， - CH = CH-基团; D是5-四唑基或-COOR 8基团，其中R 8是氢，（C 1 -C 4） - 烷基或苯基烷基; 并且m和n是0和4之间的整数。所述化合物显示白三烯拮抗活性，并且它们作为抗炎和抗过敏药物是有价值的，或用于治疗心血管疾病。

9. 发明申请

WO1997024331A1 NAPHTHALENE QUINOLINES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION 审中-公开
标题翻译：具有白藜芦醇拮抗作用的萘醌
公开(公告)号：WO1997024331A1
公开(公告)日：1997-07-10
申请号：PCT/EP1996005811
申请日：1996-12-23
申请人： LABORATORIOS MENARINI S.A. , CARGANICO, Germano , MAULEON CASELLAS, David , PASCUAL AVELLANA, Jaime , GARCIA PEREZ, Mª, Luisa , PALOMER BENET, Albert
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07D215/14
CPC分类号： C07D215/14 , C07C17/14 , C07C205/54 , C07C25/13
摘要： The present invention relates to novel naphthalene quinolines of formula (I), wherein the substituent containing A is bound to the 6- or 7-position of the 2-naphthol system; -R , R , R are independently hydrogen, fluorine, chlorine, bromine, -OCH3 or (C1-C4)-alkyl; R is hydrogen or methyl; R , R are independently hydrogen, -OH, -NH2, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylamino, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylcarbonylamino, (C1-C4)-alkoxycarbonylalkyl, carbamoyl, carbamoylalkyl, N,N-dialkylcarbamoylalkyl; -A- is a diradical -O-, -S-, -SO2-, -SO-, -SO2NR - or -NR SO2- wherein R is hydrogen or (C1-C4)-alkyl; B is a sulfur or oxygen atom or a -SO2- or -SO- group or a single bond; D is a 5-tetrazolyl or -COOR group, wherein R is hydrogen, a (C1-C4)-alkyl; or a phenylalkyl group of less than 10 carbon atoms; m is an integer from 0 to 4; n and p are integers from 0 to 6, with the proviso that n + p is less or equal to 6. Said compounds show a leukotriene-antagonistic activity, and they are valuable as anti-inflammatory and antiallergic medicaments or in the treatment of cardiovascular diseases.
摘要翻译：本发明涉及式（I）的新型萘喹啉，其中含有A的取代基与2-萘酚体系的6-位或7-位结合; -R 1，R 2，R 6独立地是氢，氟，氯，溴，-OCH 3或（C 1 -C 4） - 烷基; R 3是氢或甲基; R 4，R 5独立地是氢，-OH，-NH 2，（C 1 -C 4） - 烷基，（C 1 -C 4） - 烷氧基，（C 1 -C 4） - 烷基氨基，（C 1 -C 4） - 烷氧基羰基，（C 1 -C 4） - 烷基羰基氨基，（C 1 -C 4） - 烷氧基羰基烷基，氨基甲酰基，氨基甲酰基烷基，N，N-二烷基氨基甲酰基烷基; -A-是二价-O - ， - S - ， - SO 2 - ， - SO - ， - SO 2 NR 7 - 或-NR 7 SO 2 - 其中R 7是氢或（C 1 -C 4） - 烷基; B是硫或氧原子或-SO 2 - 或-SO-基团或单键; D是5-四唑基或-COOR 8基团，其中R 8是氢，（C 1 -C 4） - 烷基; 或小于10个碳原子的苯基烷基; m为0〜4的整数; n和p是0至6的整数，条件是n + p小于或等于6.所述化合物显示白三烯拮抗活性，并且它们作为抗炎和抗过敏药物是有价值的，或用于治疗心血管疾病。

10. 发明申请

WO1996004267A1 NAPHTHALENE AMIDES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION 审中-公开
标题翻译：具有白藜芦醇拮抗作用的萘二甲酰胺
公开(公告)号：WO1996004267A1
公开(公告)日：1996-02-15
申请号：PCT/EP1995002970
申请日：1995-07-27
申请人： LABORATORIOS MENARINI S.A. , MAULEON CASELLAS, David , CARGANICO, Germano , FOS TORRO, María de los Desamparados , GARCIA PEREZ, María Luisa , PALOMER BENET, Albert
发明人： LABORATORIOS MENARINI S.A.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D215/14 , C07D215/18
摘要： Naphthalene amides of formula (I) wherein the substituent containing A is bound to the 6- or 7- position of the 2-naphthol system; the substituent containing B is bound to the benzene ring at any free position; R is hydrogen or methyl; R is hydrogen, fluorine, chlorine or -OCH3, which is bound to the naphthalene system at any positions except the 2- and the one occupied by the other substituent; R is hydrogen, fluorine, chlorine or bromine; A- is -CO-NR - or -NR -CO- group, wherein R is hydrogen or methyl; B is a 5-tetrazolyl or -COOR group, wherein R is hydrogen, a (C1-C4)-alkyl or a phenylalkyl group of less than 10 carbon atoms; m is 0 or 1; n and p are integers from 0 to 6, with the proviso that n + p is less or equal to 6; as well as the solvates and pharmaceutically acceptable salts thereof, have leukotriene antagonistic action.
摘要翻译：式（I）的萘酰胺，其中含有A的取代基与2-萘酚体系的6-或7-位结合; 含有B的取代基在任何自由位与苯环结合; R 1是氢或甲基; R 2是氢，氟，氯或-OCH 3，其在除了2-和被另一取代基占据的任何位置之外的任何位置与萘体系结合; R 3是氢，氟，氯或溴; A是-CO-NR 4 - 或-NR 4 -CO-基，其中R 4是氢或甲基; B是5-四唑基或-COOR 5基团，其中R 5是氢，少于10个碳原子的（C 1 -C 4） - 烷基或苯基烷基; m为0或1; n和p是0至6的整数，条件是n + p小于或等于6; 以及其溶剂合物和药学上可接受的盐具有白三烯拮抗作用。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式