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![1,4-diazabicylo[3,2,2]nonane derivatives, their preparation and their therapeutic application](/abs-image/US/2002/06/18/US06407095B1/abs.jpg.150x150.jpg)
1.发明授权1,4-diazabicylo[3,2,2]nonane derivatives, their preparation and their therapeutic application 有权1,4-二氮杂双环[3,2,2]壬烷衍生物，其制备及其治疗应用公开(公告)号：US06407095B1
公开(公告)日：2002-06-18
申请号：US09856945
申请日：2001-07-16
申请人： Alistair Lochead , Samir Jegham , Alain Nedelec , Frédéric Galli , Jean Jeunesse , Luc Even
发明人： Alistair Lochead , Samir Jegham , Alain Nedelec , Frédéric Galli , Jean Jeunesse , Luc Even
IPC分类号： C07D47108
CPC分类号： C07D471/08
摘要： The invention relates to 1,4-diazabicyclo[3.2.2]nonane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.
摘要翻译： 本发明涉及1,4-二氮杂双环[3.2.2]壬烷衍生物，含有它们的药物组合物，以及用于治疗或预防与利用它们的烟碱受体功能障碍相关的病症的方法。
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![2,5,-diazabicyclo[2.2.1]heptane derivatives, their preparation and therapeutic uses](/abs-image/US/2003/10/21/US06635645B1/abs.jpg.150x150.jpg)
2.发明授权2,5,-diazabicyclo[2.2.1]heptane derivatives, their preparation and therapeutic uses 有权2,5， - 二氮杂双环[2.2.1]庚烷衍生物，其制备和治疗用途公开(公告)号：US06635645B1
公开(公告)日：2003-10-21
申请号：US09856946
申请日：2001-08-16
申请人： Alistair Lochead , Samir Jegham , Alain Nedelec , Jean Jeunesse , Frédéric Galli , Luc Even
发明人： Alistair Lochead , Samir Jegham , Alain Nedelec , Jean Jeunesse , Frédéric Galli , Luc Even
IPC分类号： C07D48708
CPC分类号： C07D487/08
摘要： The invention relates to 2,5-diazabicyclo[2.2.1]heptane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.
摘要翻译： 本发明涉及2,5-二氮杂双环[2.2.1]庚烷衍生物，含有它们的药物组合物，以及用于治疗或预防与利用它们的烟碱受体功能障碍相关的病症的方法。
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3.发明授权3-(Pyrrolidin-3-yl)-1,3,4-oxadiazol-2(3H)-one derivatives and their use as 5-HT4 ligands 失效3-（吡咯烷-3-基）-1,3,4-恶二唑-2（3H） - 酮衍生物及其作为5-HT 4配体的用途公开(公告)号：US06248757B1
公开(公告)日：2001-06-19
申请号：US09403779
申请日：1999-11-04
申请人： Alistair Lochead , Samir Jegham , Jean Jeunesse
发明人： Alistair Lochead , Samir Jegham , Jean Jeunesse
IPC分类号： A61K31445
CPC分类号： C07D413/04 , C07D413/14
摘要： Compounds corresponding to the general formula (I) in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula —OCH2O—, —O(CH2)2—, —O(CH2)3—, —O(CH2)2O— or —O(CH2)3O—, X2 represents hydrogen, an amino group or a group of general formula —NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.
摘要翻译： 对应于通式（I）的化合物，其中R 1表示氢或烷基或环烷基甲基，X 1表示氢或卤素或烷氧基，或者OR 1和X 1一起表示式-OCH 2 O-，-O（ CH2）2-，-O（CH2）3-，-O（CH2）2O-或-O（CH2）3O-，X2表示氢，氨基或通式-NHCO2R基团，其中R表示烷基 或苯基烷基，X 3表示氢或卤素，R 2表示氢或烷基，苯基烷基或[（4-二甲基氨基）哌啶-1-基羰基]烷基。 治疗应用。
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4.发明申请PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开哌啶二甲酰胺衍生物，其制备方法及其作为脂肪酸酰胺酶水解酶抑制剂的治疗方法公开(公告)号：US20100279998A1
公开(公告)日：2010-11-04
申请号：US12834267
申请日：2010-07-12
IPC分类号： A61K31/397 , C07D211/62 , A61K31/4468 , C07D401/06 , A61K31/4545 , C07D401/12 , A61K31/4709 , A61K31/506 , A61P25/06 , A61P31/22 , A61P3/10 , A61P29/00 , A61P19/02 , A61P19/06 , A61P1/00
CPC分类号： C07D207/09 , C07D205/04 , C07D211/26 , C07D211/58
摘要： The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译： 本发明涉及哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。 这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。 通过抑制FAAH酶的代谢活性，不会产生常常负责多种疾病和其他病理状况发生的化合物，并且疾病的发病率大大降低。
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5.发明申请THERAPEUTIC USES OF DERIVATIVES OF PIPERIDINYL-AND PIPERIDINYL-ALKYL CARBAMATES 审中-公开哌啶类和哌嗪酸亚胺衍生物的治疗用途公开(公告)号：US20120004207A1
公开(公告)日：2012-01-05
申请号：US13229106
申请日：2011-09-09
IPC分类号： A61K31/495 , C07D401/12 , C07D403/12 , C07D417/12 , C07D403/14 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , A61K31/397 , A61P25/00 , A61P1/08 , A61P3/00 , A61P25/28 , A61P25/08 , A61P9/00 , A61P9/10 , A61P35/00 , A61P37/00 , A61P37/08 , A61P33/00 , A61P31/12 , A61P31/04 , A61P29/00 , A61P19/10 , A61P27/02 , A61P1/00 , A61P13/00 , C07D295/15
CPC分类号： C07D211/26 , C07D213/38 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3═CHR4CONHR5; R4═H or C1-6-alkyl; R5═H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.
摘要翻译： 对应于通式（I）的化合物：其中A = N或CR 2; R 2 = H，F，OH，CN，CF 3，C 1-6 - 烷基，C 1-6 - 烷氧基; 当A = N时，n = 2或3，m = 2; 当A = CR2时，n = 1,2或3，m = 1或2。 B =共价键或C 1-8亚烷基; R1 =任选取代的杂芳基; R3 = CHR4CONHR5; R4 = H或C 1-6 - 烷基; R5 = H，C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 - 环烷基-C 1 -C 6亚烷基; 以碱的形式，酸加成盐，水合物或溶剂化物。 其治疗用途。
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6.发明授权Piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase enzyme inhibitors 失效哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶抑制剂的治疗用途公开(公告)号：US07781590B2
公开(公告)日：2010-08-24
申请号：US11465825
申请日：2006-08-21
IPC分类号： C07D421/00 , C07D211/26
CPC分类号： C07D207/09 , C07D205/04 , C07D211/26 , C07D211/58
摘要： The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译： 本发明包括哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。 这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。 通过抑制FAAH酶的代谢活性，不会产生常常负责多种疾病和其他病理状况发生的化合物，并且疾病的发病率大大降低。
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7.发明申请Derivatives of piperidinyl-and piperazinyl-alkyl carbamates, preparation methods thereof and application of same in therapeutics 失效哌啶基和哌嗪基 - 烷基氨基甲酸酯的衍生物，其制备方法和在治疗中的应用公开(公告)号：US20060089344A1
公开(公告)日：2006-04-27
申请号：US11262211
申请日：2005-10-28
IPC分类号： A61K31/519 , A61K31/517 , A61K31/496 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D211/26 , C07D213/38 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C12-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3═CHR4CONHR5; R4═H or C1-6-alkyl; R5═H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof
摘要翻译： 对应于通式（I）的化合物：其中A = N或CR 2; R 2 -H，F，OH，CN，CF 3，C 1-6烷基，C 12〜 /烷氧基; 当A = N时，n = 2或3，m = 2; 当A = CR 2时，n = 1,2或3，m = 1或2。 B =共价键或C 1-8 - 亚烷基; R 1 =任选取代的杂芳基; R 3 -CHR 4 CONHR 5 5; R 4 -H或C 1-6 - 烷基; R 5 -H，C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 环烷基-C 1 -C 6 - 亚烷基; 以碱的形式，酸加成盐，水合物或溶剂化物。 其治疗用途
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8.发明授权Therapeutic uses of derivatives of piperidinyl- and piperazinyl-alkyl carbamates 失效哌啶基和哌嗪基 - 烷基氨基甲酸酯衍生物的治疗用途公开(公告)号：US08034818B2
公开(公告)日：2011-10-11
申请号：US11670690
申请日：2007-02-02
IPC分类号： A61K31/4965 , C07D217/22
CPC分类号： C07D211/26 , C07D213/38 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Therapeutic uses of a compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3=CHR4CONHR5; R4=H or C1-6-alkyl; R5=H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate.
摘要翻译： 对应于通式（I）的化合物的治疗用途：其中A = N或CR2; R2 = H，F，OH，CN，CF3，C1-6烷基，C1-6-烷氧基; 当A = N时，n = 2或3，m = 2; 当A = CR2时，n = 1,2或3，m = 1或2。 B =共价键或C 1-8亚烷基; R 1 =任选取代的杂芳基; R3 = CHR4CONHR5; R4 = H或C1-6烷基; R5 = H，C1-6烷基，C3-7-环烷基，C3-7-环烷基-C1-C6-亚烷基; 以碱的形式，酸加成盐，水合物或溶剂化物。
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9.发明授权Derivatives of piperidinyl-and piperazinyl-alkyl carbamates, preparation methods thereof and application of same in therapeutics 失效哌啶基和哌嗪基 - 烷基氨基甲酸酯的衍生物，其制备方法和在治疗中的应用公开(公告)号：US07214798B2
公开(公告)日：2007-05-08
申请号：US11262211
申请日：2005-10-28
IPC分类号： C07D211/32
CPC分类号： C07D211/26 , C07D213/38 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3=CHR4CONHR5; R4=H or C1-6-alkyl; R5=H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1–C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.
摘要翻译： 对应于通式（I）的化合物：其中A = N或CR 2; R 2 = H，F，OH，CN，CF 3，C 1-6烷基，C 1-6， /烷氧基; 当A = N时，n = 2或3，m = 2; 当A = CR 2时，n = 1,2或3，m = 1或2。 B =共价键或C 1-8 - 亚烷基; R 1 =任选取代的杂芳基; R 3 = CHR 4 CONHR 5 5; R 4 = H或C 1-6 - 烷基; R 5 = H，C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 环烷基-C 1 -C 6 - 亚烷基; 以碱的形式，酸加成盐，水合物或溶剂化物。 其治疗用途。
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