公开(公告)号：US6166050A

公开(公告)日：2000-12-26

申请号：US458852

申请日：1999-12-10

申请人： Louis J. Lombardo ,  Joan Sabalski

发明人： Louis J. Lombardo ,  Joan Sabalski

IPC分类号： C07C229/36 ,  C07C233/87 ,  C07C271/44 ,  C07D209/14 ,  C07D211/62 ,  C07D213/38 ,  C07D213/81 ,  C07D213/82 ,  C07D233/54 ,  C07D295/135 ,  C07D295/185 ,  C07D295/205 ,  C07D213/02 ,  A61K31/44

CPC分类号： C07D213/81 ,  C07C229/36 ,  C07C233/87 ,  C07C271/44 ,  C07C2601/04 ,  C07D209/14 ,  C07D211/62 ,  C07D213/38 ,  C07D213/82 ,  C07D233/64 ,  C07D295/135 ,  C07D295/185 ,  C07D295/205

摘要： Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.

摘要翻译： 抑制由α4β1整联蛋白（VLA-4）与其反受体VCAM-1的相互作用介导的白细胞粘附的式的化合物及其用于治疗炎症和自身免疫疾病的用途。

公开(公告)号：US20050171180A1

公开(公告)日：2005-08-04

申请号：US11035005

申请日：2005-01-13

申请人： Lynn Resnick ,  Donna Huryn ,  Joan Sabalski ,  Joshua Berkowitz ,  Anthony Kreft ,  Dennis Kubrak ,  Thomas Caggiano ,  Koi Morris

发明人： Lynn Resnick ,  Donna Huryn ,  Joan Sabalski ,  Joshua Berkowitz ,  Anthony Kreft ,  Dennis Kubrak ,  Thomas Caggiano ,  Koi Morris

IPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12 ,  C07D49/02

CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 化合物具有式Ia的结构：其中R 1是低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2， / 5> 5

公开(公告)号：US20080009480A1

公开(公告)日：2008-01-10

申请号：US11837875

申请日：2007-08-13

申请人： Annmarie Sabb ,  Robert Vogel ,  James Nelson ,  Sharon Rosenzweig-Lipson ,  Gregory Welmaker ,  Joan Sabalski

发明人： Annmarie Sabb ,  Robert Vogel ,  James Nelson ,  Sharon Rosenzweig-Lipson ,  Gregory Welmaker ,  Joan Sabalski

IPC分类号： A61K31/55 ,  A61P25/28

CPC分类号： C07D209/94 ,  A61K31/55 ,  C07D487/06

摘要： This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的化合物：其中：R 1是氢，-C（O）CH 3或1-6个碳原子的烷基; R 2和R 3各自独立地为氢，1-6个碳原子的烷基，环烷基，1-6个碳原子的烷氧基，-CH 2 1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1个碳原子的氟代烷氧基 -6个碳原子，2-7个碳原子的酰基，芳基或芳酰基; R 4和R 5各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，氟烷基，-CN，烷基 1-6个碳原子的磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的氟烷氧基，2- 7个碳原子或芳酰基; R 6和R 7各自独立地为氢，C 1 -C 6烷基或环烷基; 或其药学上可接受的盐，以及含有这些化合物的药物组合物及其使用方法，包括治疗强迫症，恐慌症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍， 肥胖，癫痫和脊髓损伤。

公开(公告)号：US20070066676A1

公开(公告)日：2007-03-22

申请号：US11602531

申请日：2006-11-21

申请人： Gregory Welmaker ,  Joan Sabalski ,  Michael Smith

发明人： Gregory Welmaker ,  Joan Sabalski ,  Michael Smith

IPC分类号： A61K31/403 ,  C07D209/82

CPC分类号： C07D209/94 ,  C07D487/06

摘要： This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R′; R′ is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.

摘要翻译： 本发明提供制备下式化合物的方法：其中R为H，烷基，酰基，芳基，芳酰基或-C（O）R'; R'是烷基或芳基; R 1，R 2，R 4和R 5是H，-OH，烷基，环烷基，烷氧基 ，卤素，氟化烷基或烷氧基，-CN，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基， 酰基，芳基或芳酰基; R 3是H，烷基，环烷基，烷氧基，氟化烷基，-NH-SO 2 - 烷基，-SO 2 -NH-烷基 ，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，芳基或芳酰基; 或其药学上可接受的盐，以及可用于合成这些化合物的新化合物。

公开(公告)号：US20050004101A1

公开(公告)日：2005-01-06

申请号：US10898029

申请日：2004-07-23

申请人： Annmarie Sabb ,  Robert Vogel ,  James Nelson ,  Sharon Rosenzweig-Lipson ,  Gregory Welmaker ,  Joan Sabalski

发明人： Annmarie Sabb ,  Robert Vogel ,  James Nelson ,  Sharon Rosenzweig-Lipson ,  Gregory Welmaker ,  Joan Sabalski

IPC分类号： A61K31/551 ,  A61K31/5517 ,  A61P3/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D209/00 ,  C07D209/94 ,  C07D243/00 ,  C07D487/06 ,  A61K31/55

CPC分类号： C07D209/94 ,  A61K31/55 ,  C07D487/06

摘要： This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

摘要翻译： 本发明提供下式的化合物：其中：R 1是氢，-C（O）CH 3或1-6个碳原子的烷基; R2和R3各自独立地为氢，1-6个碳原子的烷基，环烷基，1-6个碳原子的烷氧基，-CH2OH，氟代烷基，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺 ，1-6个碳原子的氨基，烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的氟烷氧基，2-7个碳原子的酰基，芳基或芳酰基; R4和R5各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺 ，氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的氟烷氧基，2-7个碳原子的酰基或芳酰基; R6和R7各自独立地为氢，C1-C6烷基或环烷基; 或其药学上可接受的盐，以及含有这些化合物的药物组合物及其使用方法，包括治疗强迫症，恐慌症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍， 肥胖，癫痫和脊髓损伤。