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1. 发明申请

US20070219240A1 N-substituted-azacyclylamines as histamine-3 antagonists 失效
标题翻译： N-取代的氮杂环酰胺作为组胺-3拮抗剂
公开(公告)号：US20070219240A1
公开(公告)日：2007-09-20
申请号：US11724078
申请日：2007-03-14
申请人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
发明人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
IPC分类号： A61K31/4709 , A61K31/454 , A61K31/4184 , A61K31/405 , C07D403/14
CPC分类号： C07D403/10 , C07D401/10 , C07D471/04 , C07D471/14
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。

2. 发明授权

US06313126B1 Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression 失效
标题翻译：用于治疗抑郁症的芳基哌嗪基 - 环己基吲哚衍生物
公开(公告)号：US06313126B1
公开(公告)日：2001-11-06
申请号：US09476254
申请日：1999-12-30
申请人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
发明人： Richard E. Mewshaw , Ping Zhou , Dahui Zhou , Kristin L. Meagher , Magda Asselin , Deborah A. Evrard , Adam M. Gilbert
IPC分类号： A61K31496
CPC分类号： C07D401/08 , C07D209/14 , C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04
摘要： Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
摘要翻译：提供了可用于治疗受5-羟色胺影响的神经系统疾病的化合物，其包括：R 1，R 2和R 3各自独立地为氢，卤素，CF 3，烷基，烷氧基，MeSO 2或一起可以形成5-7元碳环或杂环; R 4为氢，卤素或烷基; R 5为氢，烷基，烷基芳基或芳基; R 6为氢，卤素，CF 3，CN，脲或烷氧基; X 1，X 2和X 3为碳或 X1，X2或X3可以是氮; Y是碳或氮; Z为碳或氮; 其药学上可接受的盐。

3. 发明授权

US06221874B1 Method of treating bone loss by stimulation of calcitonin 失效
标题翻译：通过刺激降钙素治疗骨质流失的方法
公开(公告)号：US06221874B1
公开(公告)日：2001-04-24
申请号：US09303972
申请日：1999-05-03
申请人： Adam Matthew Gilbert , Gerardo Francisco , Magda Asselin
发明人： Adam Matthew Gilbert , Gerardo Francisco , Magda Asselin
IPC分类号： C07D47306
CPC分类号： C07D473/06 , A61K31/522
摘要： Compounds of the formula R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon atoms; and R4 is phenyl or naphthyl substituted with alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or NR5R6; substituted or unsubstituted phenylalkyl wherein the alkyl group contains 1 to 6 carbon atoms; substituted or unsubstituted 5 to 10 membered heteroaryl having 1 to 3 heteroatoms selected from N, S and O; substituted or unsubstituted cycloalkyl of 3 to 10 carbon atoms; or substituted or unsubstituted cycloalkylalkyl of 4 to 10 carbon atoms; provided that phenyl or naphthyl is substituted with NR5R6 when R1 and R2 is alkyl, are useful in the treatment of various disorders associated bone loss by increased transcription and elevation of plasma calcitonin levels. Such disorders include, but are not limited to: Paget's Disease, post menopausal osteoporosis, senile osteoporosis, and glucocorticoid-induced osteoporosis.
摘要翻译：式R1和R2的化合物独立地为1至6个碳原子的烷基，烯丙基或3至6个碳原子的取代的烯丙基; R3为氢，1〜6个碳原子的烷基或3〜10个碳原子的环烷基; R4为苯基或被1-6个碳原子的烷基取代的萘基，具有1-6个碳原子的烷氧基或NR5R6; 取代或未取代的苯基烷基，其中烷基含有1至6个碳原子; 取代或未取代的具有1至3个选自N，S和O的杂原子的5至10元杂芳基; 3至10个碳原子的取代或未取代的环烷基; 或取代或未取代的4-10个碳原子的环烷基烷基; 条件是当R 1和R 2为烷基时苯基或萘基被NR 5 R 6取代，可用于通过增加转录和升高血浆降钙素水平来治疗与骨丢失相关的各种疾病。这种病症包括但不限于：佩吉特氏病，绝经后骨质疏松症，老年性骨质疏松症和糖皮质激素诱导的骨质疏松症。

4. 发明授权

US07820825B2 N-substituted-azacyclylamines as histamine-3 antagonists 失效
标题翻译： N-取代的氮杂环酰胺作为组胺-3拮抗剂
公开(公告)号：US07820825B2
公开(公告)日：2010-10-26
申请号：US11724078
申请日：2007-03-14
申请人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
发明人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
IPC分类号： A61K31/41 , A61K31/415 , C07D207/00 , C07D233/00 , C07D249/00
CPC分类号： C07D403/10 , C07D401/10 , C07D471/04 , C07D471/14
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。

5. 发明授权

US07781591B2 Substituted 3-cyanopyridines as protein kinase inhibitors 有权
标题翻译：取代的3-氰基吡啶作为蛋白激酶抑制剂
公开(公告)号：US07781591B2
公开(公告)日：2010-08-24
申请号：US11818119
申请日：2007-06-13
申请人： Derek Cecil Cole , Diane Harris Boschelli , Yanong Daniel Wang , Magda Asselin , Diane Marie Joseph-McCarthy , Amarnauth Shastrie Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Nathan Tumey , Chuan S. Niu , Joan Chen
发明人： Derek Cecil Cole , Diane Harris Boschelli , Yanong Daniel Wang , Magda Asselin , Diane Marie Joseph-McCarthy , Amarnauth Shastrie Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Nathan Tumey , Chuan S. Niu , Joan Chen
IPC分类号： C07D401/14
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，水合物和酯，其中R 1，R 2和X如本文所定义。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

6. 发明申请

US20070287708A1 Substituted 3-cyanopyridines as protein kinase inhibitors 有权
标题翻译：取代的3-氰基吡啶作为蛋白激酶抑制剂
公开(公告)号：US20070287708A1
公开(公告)日：2007-12-13
申请号：US11818119
申请日：2007-06-13
申请人： Derek Cole , Diane Boschelli , Yanong Wang , Magda Asselin , Diane Joseph-McCarthy , Amarnauth Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Tumey , Chuan Niu , Joan Chen
发明人： Derek Cole , Diane Boschelli , Yanong Wang , Magda Asselin , Diane Joseph-McCarthy , Amarnauth Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Tumey , Chuan Niu , Joan Chen
IPC分类号： A61K31/5377 , A61K31/4439 , C07D413/14 , C07D405/14 , C07D409/14 , C07D403/14
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，水合物和酯，其中R 1，R 2和X如本文所定义。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

7. 发明申请

US20070270440A1 N-benzoyl- and N-benzylpyrrolidin-3-ylamines as histamine-3 antagonists 失效
标题翻译： N-苯甲酰基和N-苄基吡咯烷-3-基胺作为组胺-3拮抗剂
公开(公告)号：US20070270440A1
公开(公告)日：2007-11-22
申请号：US11804686
申请日：2007-05-18
申请人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Jin-In Kim
发明人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Jin-In Kim
IPC分类号： A61K31/52 , A61K31/519 , A61K31/517
CPC分类号： C07D207/14 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。

8. 发明申请

US20070082880A1 Thieno [2,3-B] pyridine-5-carbonitriles as protein kinase inhibitors 审中-公开
标题翻译：噻吩并[2,3-B]吡啶-5-碳腈作为蛋白激酶抑制剂
公开(公告)号：US20070082880A1
公开(公告)日：2007-04-12
申请号：US11527996
申请日：2006-09-27
申请人： Diane Boschelli , Derek Cole , Magda Asselin , Ana Barrios Sosa , Biqi Wu , Lawrence Tumey
发明人： Diane Boschelli , Derek Cole , Magda Asselin , Ana Barrios Sosa , Biqi Wu , Lawrence Tumey
IPC分类号： A61K31/55 , A61K31/4743 , C07D498/02
CPC分类号： C07D495/04
摘要： Disclosed are compounds of Formula I: wherein R1, R2, R3, R4, and X, are defined hereinbefore in the specification, which can be useful in the treatment of autoimmune and inflammatory diseases, and processes for producing said compounds.
摘要翻译：公开了式I的化合物：其中R 1，R 2，R 3，R 4，和X 4，在本说明书中定义，其可用于治疗自身免疫性和炎性疾病，以及用于制备所述化合物的方法。

9. 发明申请

US20070027160A1 Piperazine-piperidine antagonists and agonists of the 5-HT1A receptor 失效
标题翻译：哌嗪 - 哌啶拮抗剂和5-HT1A受体的激动剂
公开(公告)号：US20070027160A1
公开(公告)日：2007-02-01
申请号：US11450942
申请日：2006-06-09
申请人： Magda Asselin , George Grosu , Annmarie Sabb , Wayne Childers , Lisa Havran , Zhongqi Shen , James Bicksler , Dan Chong
发明人： Magda Asselin , George Grosu , Annmarie Sabb , Wayne Childers , Lisa Havran , Zhongqi Shen , James Bicksler , Dan Chong
IPC分类号： A61K31/496 , C07D403/14
CPC分类号： C07D403/14 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction.
摘要翻译：本发明涉及新的哌嗪 - 哌啶化合物。该化合物可用作5-HT 1A结合剂，特别是5-HT 1A受体拮抗剂和激动剂。这些化合物可用于治疗中枢神经系统疾病，如认知障碍，焦虑障碍，抑郁症和性功能障碍。

10. 发明授权

US6133273A Pyrazolopyrimidine-2,4-dione sulfonamides 失效
标题翻译：吡唑并嘧啶-2,4-二酮磺酰胺
公开(公告)号：US6133273A
公开(公告)日：2000-10-17
申请号：US304180
申请日：1999-05-03
申请人： Adam Matthew Gilbert , Zhen-jia Chen , Gerardo De La Cruz Francisco , Magda Asselin
发明人： Adam Matthew Gilbert , Zhen-jia Chen , Gerardo De La Cruz Francisco , Magda Asselin
IPC分类号： A61K31/519 , C07D487/04 , A61K31/4162
CPC分类号： C07D487/04 , A61K31/519
摘要： A compound of formula (I) ##STR1## wherein: X=N and Y=CH or X=CH and Y=NR.sub.1 and R.sub.2 are independently, straight chain alkyl of 2 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms, 4 to 10 membered heteroaryl or a moiety of the formula (CH.sub.2).sub.m -A wherein m is 1 to 9 and A is cycloalkyl of 3 to 7 carbon atoms; and R.sub.3 is a straight chain alkyl of 1 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms or 4 to 10 membered heteroaryl for use in the treatment of disorders associated with bone loss by increased transcription and elevation of plasma calcitonin levels.
摘要翻译：式（I）的化合物，其中：X = N，Y = CH或X = CH，Y = N R 1，R 2独立地为2至12个碳原子的直链烷基，3至10个碳原子的支链烷基， 3至10个碳原子的环烷基，4至10个碳原子的芳基，4至10元杂芳基或式（CH2）mA部分，其中m为1至9，A为3至7个碳原子的环烷基; 并且R 3是1至12个碳原子的直链烷基，3至10个碳原子的支链烷基，4至10个碳原子的芳基或4至10元杂芳基，用于治疗与骨丢失相关的疾病增加血浆降钙素水平的转录和升高。

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