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11. 发明申请

US20130281415A9 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING ß2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES 有权
标题翻译：具有β2ADRENERGIC AGONIST和M3 MUSCARINIC ANTAGONIST活动的新CYCLOHEXYLAMINE衍生物
公开(公告)号：US20130281415A9
公开(公告)日：2013-10-24
申请号：US13697060
申请日：2011-05-13
申请人： Maria Prat Quinones , Silvia Fonquerna Pou , Carlos Puig Duran , Wenceslao Lumeras Amador , Jose Aiguade Bosch , Juan Francisco Caturla Javaloyes
发明人： Maria Prat Quinones , Silvia Fonquerna Pou , Carlos Puig Duran , Wenceslao Lumeras Amador , Jose Aiguade Bosch , Juan Francisco Caturla Javaloyes
IPC分类号： A61K31/4709 , A61K31/56 , C07D413/14 , A61K31/538 , C07D405/12 , C07D215/26 , A61K31/4704 , C07D409/12 , A61P11/00 , A61P15/06 , A61P27/06 , A61P25/00 , A61P9/00 , A61P29/00 , A61P1/00 , A61P11/06 , C07D409/14
CPC分类号： C07D215/26 , A61K31/4709 , B29C44/1223 , C07D409/14 , Y10S514/826
摘要： The present disclosure relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
摘要翻译：本公开涉及具有β2肾上腺素能激动剂和M3毒蕈碱拮抗剂双重活性的新化合物，含有它们的药物组合物，其制备方法及其在呼吸治疗中的用途。

12. 发明申请

US20110028442A1 DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL) PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR 审中-公开
标题翻译： 4-（2-氨基-1-羟基乙基）苯酚的衍生物作为BETA2 ADRENERGIC受体的激动剂
公开(公告)号：US20110028442A1
公开(公告)日：2011-02-03
申请号：US12919134
申请日：2009-02-27
申请人： Carlos Puig Duran , Daniel Perez Crespo , Maria Isabel Crespo Crespo , Lala Sole Feu , Maria Prat Quinones
发明人： Carlos Puig Duran , Daniel Perez Crespo , Maria Isabel Crespo Crespo , Lala Sole Feu , Maria Prat Quinones
IPC分类号： A61K31/56 , C07C275/28 , A61K31/17 , A61P11/00 , A61P9/00 , A61P29/00 , A61P27/06 , A61P25/00 , C07D215/26 , A61K31/4704
CPC分类号： C07C275/40
摘要： The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.
摘要翻译：本公开涉及式（I）的4-（2-氨基-1-羟乙基）苯酚衍生物以及包含它们的药物组合物，以及它们在治疗中作为β肾上腺素能受体激动剂的用途。

13. 发明申请

US20090198064A1 Process for preparing quinuclidinium carbamate derivatives 审中-公开
标题翻译：喹喔啉铵氨基甲酸酯衍生物的制备方法
公开(公告)号：US20090198064A1
公开(公告)日：2009-08-06
申请号：US11658662
申请日：2005-07-08
申请人： Maria Prat Quinones , Nuria Busquets Baque , Ferran Pujol Noguera , Francisco Javier Ibarzo Casamian
发明人： Maria Prat Quinones , Nuria Busquets Baque , Ferran Pujol Noguera , Francisco Javier Ibarzo Casamian
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A new process for preparing carbamate derivatives having the structure of formula (I) by reacting, in a first step, a compound of formula (II) with a compound of formula (III) and reacting the product of this first step with an acylating agent of formula (V).
摘要翻译：一种制备具有式（I）结构的氨基甲酸酯衍生物的新方法，通过在第一步中使式（II）化合物与式（III）化合物反应，并将该第一步产物与酰化剂的式（Ⅴ）。

14. 发明授权

US07122558B2 Quinuclidine derivatives and medicinal compositions containing the same 失效
公开(公告)号：US07122558B2
公开(公告)日：2006-10-17
申请号：US10250447
申请日：2001-12-20
申请人： Maria Prat Quinones , Maria Dolors Fernandez Forner , Maria Antonia Buil Albero
发明人： Maria Prat Quinones , Maria Dolors Fernandez Forner , Maria Antonia Buil Albero
IPC分类号： A61K31/46 , C07D453/02
CPC分类号： C07D453/02
摘要： A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, a phenyl group, —OR7, —SR7, —NR7R8, —NHCOR7, —CONR7R8, —CN, —NO2, —COOR7 or CF3 group, or a strait or branched, substituted or unsubstituted lower alkyl group, wherein R7 and R8 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic or alicyclic ring or a heterocyclic group. n is an integer from 0 to 4; A represents a group selected from —CH2—, —CH═CR9—, —CR9═CH—, —CR9R10—, —CO—, —O—, —S—, —S(O)—, —S(O)2— and NR9, wherein R9 and R10 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; m is an integer from 0 to 8, provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azonia bicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; R4 represents a group of structure: (Formulae II) wherein R11 represents a hydrogen or halogen atom, a hydroxy group, an alkoxy group, a nitro group, a cyano group, —CO2R12 or —NR12R13, wherein R12 and R13 are identical or different and are selected from hydrogen and straight or branched lower alkyl groups, or a straight or branched, substituted or unsubstituted lower alkyl group; R5 represents an alkyl group of 1 to 7 carbon atoms, an alkenyl group containing 2 to 7 carbon atoms, or a group of formula (III) wherein q=1 or 2 and R11 iss a defined above; R6 represents a hydrogen atom, a hydroxy group, a methyl group or a —CH2OH group; and X− represents a pharmaceutically acceptable anion of a mono or polyvalent acid .

15. 发明授权

US5639904A 1-aryloxy-3-alkylamino-2-propanol nitrate esters, the use thereof and corresponding pharmaceutical composition 失效
标题翻译： 1-芳氧基-3-烷基氨基-2-丙醇硝酸酯，其用途和相应的药物组合物
公开(公告)号：US5639904A
公开(公告)日：1997-06-17
申请号：US514267
申请日：1995-08-11
申请人： Maria Prat Quinones , Joan Pi Sallent , Dagmar Vedrilla Veit
发明人： Maria Prat Quinones , Joan Pi Sallent , Dagmar Vedrilla Veit
IPC分类号： A61K31/135 , A61K31/165 , A61K31/21 , A61K31/215 , A61P9/08 , A61P9/10 , C07C217/32 , C07C235/34 , C07C205/01
CPC分类号： C07C235/34 , C07C217/32
摘要： The 1-aryloxy-3-alkylamino-2-propanol nitrate esters, having formula I: ##STR1## the enantiomers and diastereoisomers and the therapeutically acceptable salts thereof, wherein R.sub.1 is a chain of general formula II --(CH.sub.2).sub.m --Z--R.sub.2, where: m is 1 or 2; Z is an --O-- ether, --CONH amide or --COO-- ester function; and R.sub.2 is a C.sub.2-3 straight or branched chain alkyl having at least one nitroxy group as substituent; and Ar is a benzene ring when Z is the ether or ester function, and a naphthalene ring when Z is the amide function, are of use for the treatment of cardiovascular affections.
摘要翻译：具有式I的1-芳氧基-3-烷基氨基-2-丙醇硝酸酯：其中R1是通式II-（CH2）mZ的对映异构体和非对映异构体及其治疗上可接受的盐， -R2，其中：m为1或2; Z是-O-醚，-CONH酰胺或-COO-酯官能团; R2为具有至少一个硝酰氧基作为取代基的C2-3直链或支链烷基; 当Z为醚或酯官能团时，Ar为苯环，Z为酰胺官能团时为萘环，用于治疗心血管疾病。

16. 发明授权

US08513279B2 Quinuclidine derivatives and medicinal compositions containing the same 有权
标题翻译：奎宁环衍生物和含有它们的药物组合物
公开(公告)号：US08513279B2
公开(公告)日：2013-08-20
申请号：US13354873
申请日：2012-01-20
申请人： Maria Dolors Fernandez Forner , Maria Prat Quinones , Maria Antonia Buil Albero
发明人： Maria Dolors Fernandez Forner , Maria Prat Quinones , Maria Antonia Buil Albero
IPC分类号： A61K31/439 , A61K31/56
CPC分类号： A61K31/439 , A61K9/0073 , A61K9/0075 , A61K31/4745 , A61K31/56 , A61K45/06 , A61K47/26 , C07D453/02 , Y10S514/826 , A61K2300/00
摘要： The invention provides 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide in combination with a steroid, and methods of using it for treatment of respiratory disorders.
摘要翻译：本发明提供与类固醇组合的3-（2-羟基-2,2-二噻吩-2-基乙酰氧基）-1-（3-苯氧基丙基）-1-氮鎓双环[2.2.2]辛烷和其使用方法用于治疗呼吸系统疾病。

17. 发明授权

US07893087B2 Quinuclidine derivatives and medicinal compositions containing the same 失效
标题翻译：奎宁环衍生物和含有它们的药物组合物
公开(公告)号：US07893087B2
公开(公告)日：2011-02-22
申请号：US11515335
申请日：2006-08-31
申请人： Maria Prat Quinones , Maria Dolors Fernandez Forner , Maria Antonia Buil Albero
发明人： Maria Prat Quinones , Maria Dolors Fernandez Forner , Maria Antonia Buil Albero
IPC分类号： A61K31/4745 , A61K31/407 , A61K31/4178 , C07D453/02
CPC分类号： C07D453/02
摘要： A compound of formula (I) is provided, wherein B, A, R1, R2, R3, R4, R5 and R6 are as defined herein and X− represents a pharmaceutically acceptable anion of a mono or polyvalent acid. Processes for the preparation of such compounds and pharmaceutical compositions containing them are also provided.
摘要翻译：提供式（I）化合物，其中B，A，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义，X - 表示单价或多价酸的药学上可接受的阴离子。还提供了制备这些化合物的方法和含有它们的药物组合物。

18. 发明授权

US07776879B2 Quinuclidine carbamate derivatives and their use as M3 antagonists 失效
标题翻译：奎宁环氨基甲酸酯衍生物及其作为M3拮抗剂的用途
公开(公告)号：US07776879B2
公开(公告)日：2010-08-17
申请号：US11806927
申请日：2007-06-05
申请人： Maria Antonia Buil Albero , Maria Dolors Fernandez Forner , Maria Prat Quinones
发明人： Maria Antonia Buil Albero , Maria Dolors Fernandez Forner , Maria Prat Quinones
IPC分类号： A61K31/439 , A61P1/00 , A61P11/00 , A61P13/00 , C07D453/02
CPC分类号： C07D471/08 , C07D453/02
摘要： A carbamate of formula (I), wherein R1 represents wherein R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 or 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicylic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof. The pharmaceutically acceptable salt may be of formula (II).
摘要翻译：式（I）的氨基甲酸酯，其中R 1表示其中R 2表示苄基，苯乙基，呋喃-2-基甲基，呋喃-3-基甲基，噻吩-2-基甲基或噻吩-3-基甲基或直链或支链烷基具有3或8个碳原子，具有3至8个碳原子的烯基或3至6个碳原子的环烷基; p是1或2，并且在氮杂烷环中的取代可以在2,3或4位，包括不对称碳的所有可能的构型; 或其药学上可接受的盐。药学上可接受的盐可以是式（II）。

19. 发明授权

US07718670B2 Quinuclidine amide derivatives 失效
标题翻译：奎宁环酰胺衍生物
公开(公告)号：US07718670B2
公开(公告)日：2010-05-18
申请号：US11970698
申请日：2008-01-08
申请人： Maria Prat Quinones
发明人： Maria Prat Quinones
IPC分类号： A61K31/439 , A61P11/00 , C07D453/06
CPC分类号： C07D487/08 , C07D453/02
摘要： New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.
摘要翻译：公开了具有通式（I）的化学结构的新的奎宁环酰胺衍生物及其药学上可接受的盐，包括式（II）的季盐; 以及其制备方法，包含它们的药物组合物及其在治疗中作为M3毒蕈碱受体的拮抗剂的用途。

20. 发明申请

US20080221155A1 Novel quinuclidine derivatives and medicinal compositions containing the same 有权
公开(公告)号：US20080221155A1
公开(公告)日：2008-09-11
申请号：US12074929
申请日：2008-03-07
申请人： Maria Dolors Fernandez Forner , Maria Prat Quinones , Maria Antonia Buil Albero
发明人： Maria Dolors Fernandez Forner , Maria Prat Quinones , Maria Antonia Buil Albero
IPC分类号： A61K31/46 , A61P11/00
CPC分类号： A61K31/439 , A61K9/0073 , A61K9/0075 , A61K31/4745 , A61K31/56 , A61K45/06 , A61K47/26 , C07D453/02 , Y10S514/826 , A61K2300/00
摘要： A compound according to formula (I) wherein: © is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; m is an integer from 0 to 8; provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; B represents a group of formula i) or ii): wherein R10 represents a hydrogen atom, a hydroxy or methyl group; and R8 and R9 each independently represents wherein R11 represents a hydrogen or halogen atom, or a straight or branched lower alkyl group and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and when i) or ii) contain a chiral centre they may represent either configuration; X represents a pharmaceutically acceptable anion of a mono or polyvalent acid, which shows high affinity for muscarinic M3 receptors (Hm3).

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