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1. 发明申请

US20060229304A1 (R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效
公开(公告)号：US20060229304A1
公开(公告)日：2006-10-12
申请号：US11373770
申请日：2006-03-09
申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号： A61K31/538 , C07D265/36 , A61K31/138
CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.

2. 发明申请

US20050043294A1 (R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效
标题翻译：（R） - 用于抑制胆固醇酯转移蛋白活性的卤代取代稠合杂环氨基化合物
公开(公告)号：US20050043294A1
公开(公告)日：2005-02-24
申请号：US10929013
申请日：2004-08-27
申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号： C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07D213/65 , C07D251/42 , C07D307/42 , C07D333/20 , A61K31/55 , A61K31/137 , A61K31/47
CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
摘要翻译：本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代的芳基和杂芳基（R） - 手性卤代1-取代氨基 - （n + 1） - 阿尔卡醇化合物，化合物，组合物和方法用于治疗动脉粥样硬化和其他冠状动脉疾病。描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。

3. 发明申请

US20070219274A1 (R)-Chiral Halogenated Substituted Fused Heterocyclic Amino Compounds Useful for Inhibiting Cholesterol Ester Transfer Protein Activity 审中-公开
标题翻译：（R） - 用于抑制胆固醇酯转移蛋白活性的手性卤代取代的稠合杂环氨基化合物
公开(公告)号：US20070219274A1
公开(公告)日：2007-09-20
申请号：US11693161
申请日：2007-03-29
申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号： A61K31/135 , C07C211/43
CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
摘要翻译：本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代的芳基和杂芳基（R） - 手性卤代1-取代氨基 - （n + 1） - 阿尔卡醇化合物，化合物，组合物和方法用于治疗动脉粥样硬化和其他冠状动脉疾病。描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。

4. 发明申请

US20070213376A1 Halogenated sulfonamide derivatives 审中-公开
标题翻译：卤代磺酰胺衍生物
公开(公告)号：US20070213376A1
公开(公告)日：2007-09-13
申请号：US11714008
申请日：2007-03-05
申请人： Vrej Jubian , Mathivanan Packiarajan , Emily Reinhard
发明人： Vrej Jubian , Mathivanan Packiarajan , Emily Reinhard
IPC分类号： A61K31/44
CPC分类号： C07D417/04
摘要： This invention is directed to halogenated sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from anxiety which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, the present invention is directed to use of a compound of the invention for the manufacture of a medicament for treating a subject suffering from depression, anxiety or obesity.
摘要翻译：本发明涉及作为NPY Y5受体的配体的卤代磺酰胺衍生物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了治疗患有抑郁症的受试者的方法，其包括给予受试者一定量的本发明化合物。本发明还提供了治疗患有焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。本发明还提供了治疗患有肥胖症的受试者的方法，其包括给予受试者一定量的本发明化合物。此外，本发明涉及本发明化合物在制备用于治疗患有抑郁，焦虑或肥胖的受试者的药物中的用途。

5. 发明申请

US20070054901A1 Dihydrothiazine prodrugs of thiazolium agents 失效
标题翻译：噻唑类药物的二氢噻嗪前药
公开(公告)号：US20070054901A1
公开(公告)日：2007-03-08
申请号：US11390946
申请日：2006-03-27
申请人： Emily Reinhard , Elliot Katten
发明人： Emily Reinhard , Elliot Katten
IPC分类号： A61K31/54 , A61K31/541 , A61K31/426 , C07D279/12
CPC分类号： C07D279/12
摘要： Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or α-hydroxyethyl; R1 and R2 are independently selected from hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C8 cycloalkyl, C1-C6 alkenyl, C1-C6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C1-C6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R1 and R2 is other than hydrogen, and (b) if R2 is hydrogen R1 is other than methyl. Also provided are pharmaceutical compositions containing the compounds, and methods for the preparation of the compounds. The compounds are useful, among other things, as prodrugs which can be converted under acidic conditions to thiazolium agents. The compounds can be administered to mammals, including humans, for treatment of various indications.
摘要翻译：本发明提供下式的化合物及其药学上可接受的盐：其中：R是氢，甲基，羟甲基或α-羟乙基; R 1和R 2独立地选自氢，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6 - 羟基烷基，C 3 -C 8环烷基，C 1 -C 3 - C 1 -C 6亚烷基，C 1 -C 6炔基，氨基，单烷基氨基，二烷基氨基烷基和吡咯烷-1-基烷基; 并且Y选自C 1 -C 6烷基，取代和未取代的芳基; 条件是：（a）如果Y是芳基，那么R 1和R 2中的至少一个不是氢，和（b）如果R SUP > 2 是氢R 1以外的是甲基。还提供含有这些化合物的药物组合物，以及制备化合物的方法。所述化合物尤其可用作可在酸性条件下转化为噻唑鎓试剂的前药。化合物可以施用于哺乳动物，包括人类，用于治疗各种适应症。

6. 发明授权

US07511036B2 Dihydrothiazine prodrugs of thiazolium agents 失效
标题翻译：噻唑类药物的二氢噻嗪前药
公开(公告)号：US07511036B2
公开(公告)日：2009-03-31
申请号：US11390946
申请日：2006-03-27
申请人： Emily Reinhard , Elliot Katten
发明人： Emily Reinhard , Elliot Katten
IPC分类号： C07D279/12 , A61K31/54 , A61K31/541 , A61K31/426
CPC分类号： C07D279/12
摘要： Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or α-hydroxyethyl; R1 and R2 are independently selected from hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C8 cycloalkyl, C1-C6 alkenyl, C1-C6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C1-C6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R1 and R2 is other than hydrogen, and (b) if R2 is hydrogen R1 is other than methyl. Also provided are pharmaceutical compositions containing the compounds, and methods for the preparation of the compounds. The compounds are useful, among other things, as prodrugs which can be converted under acidic conditions to thiazolium agents. The compounds can be administered to mammals, including humans, for treatment of various indications.
摘要翻译：本发明提供下式的化合物及其药学上可接受的盐：其中：R是氢，甲基，羟甲基或α-羟乙基; R 1和R 2独立地选自氢，C 1 -C 6烷基，C 1 -C 6羟基烷基，C 3 -C 8环烷基，C 1 -C 6烯基，C 1 -C 6炔基，氨基，单烷基氨基，二烷基氨基烷基和吡咯烷-1-基烷基; Y选自C1-C6烷基，取代和未取代的芳基; 条件是：（a）如果Y是芳基，则R 1和R 2中的至少一个不是氢，和（b）如果R 2是氢，则R 1不是甲基。还提供含有这些化合物的药物组合物，以及制备化合物的方法。所述化合物尤其可用作可在酸性条件下转化为噻唑鎓试剂的前药。化合物可以施用于哺乳动物，包括人类，用于治疗各种适应症。

7. 发明申请

US20050014747A1 Dihydrothiazine prodrugs of thiazolium agents 审中-公开
标题翻译：噻唑类药物的二氢噻嗪前药
公开(公告)号：US20050014747A1
公开(公告)日：2005-01-20
申请号：US10824848
申请日：2004-04-15
申请人： Emily Reinhard , Elliot Katten
发明人： Emily Reinhard , Elliot Katten
IPC分类号： A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , C07D279/12 , A61K31/54 , A61K31/541
CPC分类号： C07D279/12
摘要： Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or α-hydroxyethyl; R1 and R2 are independently selected from hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C8 cycloalkyl, C1-C6 alkenyl, C1-C6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C1-C6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R1 and R2 is other than hydrogen, and (b) if R2 is hydrogen R1 is other than methyl. Also provided are pharmaceutical compositions containing the compounds, and methods for the preparation of the compounds. The compounds are useful, among other things, as prodrugs which can be converted under acidic conditions to thiazolium agents. The compounds can be administered to mammals, including humans, for treatment of various indications.
摘要翻译：本发明提供下式的化合物及其药学上可接受的盐：其中：R是氢，甲基，羟甲基或α-羟乙基; R 1和R 2独立地选自氢，C 1 -C 6烷基，C 1 -C 6羟基烷基，C 3 -C 8环烷基，C 1 -C 6烯基，C 1 -C 6炔基，氨基，单烷基氨基，二烷基氨基烷基和吡咯烷-1 - 烷基; Y选自C1-C6烷基，取代和未取代的芳基; 条件是：（a）如果Y是芳基，则R 1和R 2中的至少一个不是氢，和（b）如果R 2是氢，则R 1不是甲基。还提供含有这些化合物的药物组合物，以及制备化合物的方法。所述化合物尤其可用作可在酸性条件下转化为噻唑鎓试剂的前药。化合物可以施用于哺乳动物，包括人类，用于治疗各种适应症。

8. 发明申请

US20060293341A1 Alkyl sulfonamide derivatives 审中-公开
标题翻译：烷基磺酰胺衍生物
公开(公告)号：US20060293341A1
公开(公告)日：2006-12-28
申请号：US11472826
申请日：2006-06-21
申请人： Vrej Jubian , Mathivanan Packiarajan , Hermogenes Jimenez , Emily Reinhard
发明人： Vrej Jubian , Mathivanan Packiarajan , Hermogenes Jimenez , Emily Reinhard
IPC分类号： A61K31/497 , A61K31/4439 , C07D417/02
CPC分类号： C07D417/04
摘要： This invention is directed to alkyl sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from anxiety which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention.
摘要翻译：本发明涉及作为NPY Y5受体的配体的烷基磺酰胺衍生物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了治疗患有抑郁症的受试者的方法，其包括给予受试者一定量的本发明化合物。本发明还提供了治疗患有焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。本发明还提供了治疗患有肥胖症的受试者的方法，其包括给予受试者一定量的本发明化合物。

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