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1. 发明授权

US06476038B1 Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines 失效
标题翻译：氨基取代的吡唑并[1,5-a] -1,5-嘧啶和吡唑并[1,5-a] -1,3,5-三嗪
公开(公告)号：US06476038B1
公开(公告)日：2002-11-05
申请号：US09676972
申请日：2000-09-29
申请人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
发明人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
IPC分类号： C07D48704
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。这些化合物是NPY1受体的选择性调节剂。这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。给出了在受体定位研究中使用化合物的方法。

2. 发明授权

US07074929B2 Certain alkylene diamine-substituted heterocycles 失效
标题翻译：某些亚烷基二胺取代的杂环
公开(公告)号：US07074929B2
公开(公告)日：2006-07-11
申请号：US10705446
申请日：2003-11-10
申请人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D471/04 , A61K31/4375 , A61P15/10 , A61P3/04
CPC分类号： C07D213/73 , C07D215/46 , C07D239/48 , C07D471/04 , C07D471/14 , C07D473/34 , C07D475/08 , C07D487/04 , C07D495/04 , G01N2333/5755 , G01N2333/70571
摘要： This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and XI
摘要翻译：本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。本发明包括的新化合物是式II，IV，V，VII-IX和XI的化合物

3. 发明授权

US06566367B2 Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines 失效
公开(公告)号：US06566367B2
公开(公告)日：2003-05-20
申请号：US10013846
申请日：2001-12-11
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry L. Brielmann , James William Darrow , Stéphane De Lombaert , Alan Hutchison , Jennifer Tran , Xiaozhang Zheng , Richard Louis Elliott , Marlys Hammond
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry L. Brielmann , James William Darrow , Stéphane De Lombaert , Alan Hutchison , Jennifer Tran , Xiaozhang Zheng , Richard Louis Elliott , Marlys Hammond
IPC分类号： C07D47110
CPC分类号： C07D487/04 , C07D491/10
摘要： Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

4. 发明授权

US06506762B1 Certain alkylene diamine-substituted heterocycles 失效
标题翻译：某些亚烷基二胺取代的杂环
公开(公告)号：US06506762B1
公开(公告)日：2003-01-14
申请号：US09676941
申请日：2000-09-29
申请人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D48704
CPC分类号： C07D213/73 , C07D215/46 , C07D239/48 , C07D471/04 , C07D471/14 , C07D473/34 , C07D475/08 , C07D487/04 , C07D495/04 , G01N2333/5755 , G01N2333/70571
摘要： The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C═O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonded to L or J, or O, S, C═O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; the 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C═O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.
摘要翻译：本发明还提供了通用方法，其中单环，双环或三环杂环可以被修饰以在NPY1受体上获得有效的拮抗剂。本发明提供NPY受体的新型有效的非肽拮抗剂，特别是 NPY1受体由选自单，双或三环杂环核心设计。本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。包含的新化合物本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR15; Y为N或CR 3; E，F和G各自独立地为CR 3或N; 当双键连接到相邻的环原子时，当单键连接到两个相邻的环原子，或N或CR 3时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15;当双键键合时，K为N或CR 3 当与两个相邻的环原子单键键合时，或当与相邻环原子双键键合时为N或CR 3，L或J，或O，S，C = O，CR 3 R 16或NR 15;当单键连接到所有相邻环原子时，L为N或CR16 当与K键合时，其连接的原子或C（碳）;含有I，J，K和L的6-或7-元环可以含有1至3个双键，0至2个杂原子和0〜2个C = O基团，其中这些基团的碳原子是环的一部分，氧原子是环上的取代基; Q是O或NR15。这些化合物抑制神经肽Y在这些受体上的活性可用于治疗与过量神经肽Y相关的生理紊乱，包括进食障碍，例如肥胖症和贪食症，以及某些心血管疾病，例如高血压。

5. 发明申请

US20100029637A1 Chymase Inhibitors 有权
标题翻译：糜酶抑制剂
公开(公告)号：US20100029637A1
公开(公告)日：2010-02-04
申请号：US12443498
申请日：2007-09-27
申请人： Stéphane De Lombaert , Michel Jose Emmanuel
发明人： Stéphane De Lombaert , Michel Jose Emmanuel
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61P9/00
CPC分类号： C07D471/04
摘要： Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
摘要翻译：公开了可用于治疗涉及胃促胰酶的各种疾病和病症的小分子抑制剂。

6. 发明授权

US07329664B2 Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues 失效
标题翻译：取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物
公开(公告)号：US07329664B2
公开(公告)日：2008-02-12
申请号：US10892741
申请日：2004-07-16
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Stéphane De Lombaert , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Stéphane De Lombaert , Xiaozhang Zheng
IPC分类号： A61K31/517 , A61K31/519 , C07D401/04 , C07D405/14 , C07D487/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies
摘要翻译：提供了取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法

7. 发明授权

US07304059B2 Substituted quinazolin-4-ylamine analogues 有权
标题翻译：取代的喹唑啉-4-基胺类似物
公开(公告)号：US07304059B2
公开(公告)日：2007-12-04
申请号：US11345926
申请日：2006-02-01
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane De Lombaert , Kevin J. Hodgetts , Xiaozhang Zheng , Taeyoung Yoon
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane De Lombaert , Kevin J. Hodgetts , Xiaozhang Zheng , Taeyoung Yoon
IPC分类号： C07D403/12 , C07D403/14 , A61K31/517
CPC分类号： C07D401/04 , C07D215/42 , C07D215/44 , C07D237/34 , C07D239/94 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D419/14 , C07D471/04
摘要： Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了取代的喹唑啉-4-基胺类似物。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

8. 发明授权

US06696445B2 Certain alkylene diamine-substituted heterocycles 失效
标题翻译：某些亚烷基二胺取代的杂环
公开(公告)号：US06696445B2
公开(公告)日：2004-02-24
申请号：US10291446
申请日：2002-11-08
申请人： Raymond F. Horvath , Jennifer N Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer N Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D40112
CPC分类号： C07D213/73 , C07D215/46 , C07D239/48 , C07D471/04 , C07D471/14 , C07D473/34 , C07D475/08 , C07D487/04 , C07D495/04 , G01N2333/5755 , G01N2333/70571
摘要： The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C═O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonded to L or J, or O, S, C═O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; The 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C═O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.
摘要翻译：本发明还提供了通用方法，其中单环，双环或三环杂环可以被修饰以在NPY1受体上获得有效的拮抗剂。本发明提供NPY受体的新型有效的非肽拮抗剂，特别是 NPY1受体由选自单，双或三环杂环核心设计。本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。包含的新化合物通过本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR 15; Y是N或CR 3; E，F和G各自独立地为CR 3或N; 当单键结合到两个相邻的环原子上时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15，当双键键合到相邻的环原子;当双键连接到L或J或O，S，C = O，CR 3 R 16或NR 15时，K是N或CR 3。当与相邻的环原子双键键合时，N或CR 3，当与其连接的所有原子单键键合时，L是N或CR 16，或当双键键合到K时，C（碳）; 含有I，J，K和L的6-或7-元环可以含有1至3个双键，0至2个杂原子和0至2个C = O基团，其中这些基团的碳原子是环的一部分，氧原子是环上的取代基; Q是O或NR 15。这些化合物抑制神经肽Y在那些受体上的活性可用于治疗与过量神经肽Y相关的生理障碍，包括进食障碍，例如肥胖和贪食症，以及某些心脏病高血压等疾病。

9. 发明申请

US20090286767A1 SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES 审中-公开
标题翻译：取代喹啉-4-甲胺类似物
公开(公告)号：US20090286767A1
公开(公告)日：2009-11-19
申请号：US12368302
申请日：2009-02-09
申请人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
发明人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
IPC分类号： A61K31/397 , C12N5/00 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/4375 , A61K31/4709 , C07D413/14 , C07D405/14 , C07D401/14 , C07D401/10 , A61P3/04 , A61P29/00
CPC分类号： C07D401/04 , C07D215/44 , C07D471/04 , C07D491/14
摘要： Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供取代的喹啉-4-基胺类似物。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

10. 发明授权

US07488740B2 Substituted quinolin-4-ylamine analogues 失效
标题翻译：取代的喹啉-4-基胺类似物
公开(公告)号：US07488740B2
公开(公告)日：2009-02-10
申请号：US10891832
申请日：2004-07-14
申请人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
发明人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
IPC分类号： A61K31/47 , C07D215/38
CPC分类号： C07D401/04 , C07D215/44 , C07D471/04 , C07D491/14
摘要： Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供取代的喹啉-4-基胺类似物。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

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