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1. 发明授权

US07943658B2 Indole indane amide compounds useful as CB2 agonists and method 有权
标题翻译：用作CB2激动剂的吲哚吲哚酰胺化合物和方法
公开(公告)号：US07943658B2
公开(公告)日：2011-05-17
申请号：US12177319
申请日：2008-07-22
申请人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
发明人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/42 , C07D413/06
摘要： Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
摘要翻译：提供了CB2激动剂的吲哚二氢化茚酰胺，其具有其中R 1，R 2，R 3，R 4和R 5如本文所定义的结构，该化合物可用于治疗由CB2受体介导的自身免疫疾病，炎症，疼痛，心血管疾病和其它疾病。还提供了使用本发明化合物预防或治疗这些疾病的方法。

2. 发明申请

US20090041722A1 INDOLE INDANE AMIDE COMPOUNDS USEFUL AS CB2 AGONISTS AND METHOD 有权
标题翻译：单独使用吲哚类化合物作为CB2激发剂和方法有用
公开(公告)号：US20090041722A1
公开(公告)日：2009-02-12
申请号：US12177319
申请日：2008-07-22
申请人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
发明人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
IPC分类号： A61K31/404 , C07D209/42 , A61K31/5377 , A61P11/00 , A61P25/00 , A61K38/21 , C07D413/06
CPC分类号： C07D209/42 , C07D413/06
摘要： Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
摘要翻译：提供了CB2激动剂的吲哚二氢化茚酰胺，其具有其中R 1，R 2，R 3，R 4和R 5如本文所定义的结构，该化合物可用于治疗由CB2受体介导的自身免疫疾病，炎症，疼痛，心血管疾病和其它疾病。还提供了使用本发明化合物预防或治疗这些疾病的方法。

3. 发明申请

US20080228055A1 Fluctuating Blood Glucose Notification Threshold Profiles and Methods of Use 有权
标题翻译：波动血糖通知阈值配置文件和使用方法
公开(公告)号：US20080228055A1
公开(公告)日：2008-09-18
申请号：US10589211
申请日：2006-06-08
申请人： Philip M. Sher
发明人： Philip M. Sher
IPC分类号： A61B5/00
CPC分类号： A61B5/14532 , A61B5/7275 , G06F19/00
摘要： Embodiments of the present invention provide a new system and methods for monitoring blood glucose concentration. A user of a continuous glucose monitor may program upper and lower blood glucose notification thresholds to fluctuate over time in order to facilitate management of the short-term effects of food consumption, insulin delivery aberrations, physical activity, emotions, and unforeseen circumstances.
摘要翻译：本发明的实施例提供了一种用于监测血糖浓度的新系统和方法。连续葡萄糖监测器的用户可以对上下血糖通知阈值进行编程以随时间变化，以便于管理食物消耗，胰岛素输送畸变，身体活动，情绪和不可预见情况的短期影响。

4. 发明授权

US5541204A Aryloxypropanolamine .beta. 3 adrenergic agonists 失效
标题翻译： Aryloxypropanolamine beta 3肾上腺素能激动剂
公开(公告)号：US5541204A
公开(公告)日：1996-07-30
申请号：US352824
申请日：1994-12-02
申请人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
发明人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/215 , A61K31/275 , A61K31/357 , A61K31/36 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/47 , A61P1/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P25/02 , A61P43/00 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C311/08 , C07C317/32 , C07C317/36 , C07D209/42 , C07D215/22 , C07D215/227 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12
CPC分类号： C07D215/227 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C317/32 , C07D209/42 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.
摘要翻译：式I化合物及其药学上可接受的盐，其中：R 1至R 9如本文所定义，m为0或1的整数。这些化合物为β3肾上腺素能受体激动剂，因此可用于例如治疗的糖尿病，肥胖，胃肠道疾病和贲门失弛缓症。

5. 发明授权

US07452892B2 Triazolopyrimidine cannabinoid receptor 1 antagonists 有权
标题翻译：三唑并嘧啶大麻素受体1拮抗剂
公开(公告)号：US07452892B2
公开(公告)日：2008-11-18
申请号：US11455083
申请日：2006-06-16
申请人： Gang Wu , Amarendra B. Mikkilineni , Philip M. Sher , Natesan Murugesan , Zhengxiang Gu
发明人： Gang Wu , Amarendra B. Mikkilineni , Philip M. Sher , Natesan Murugesan , Zhengxiang Gu
IPC分类号： A61K31/519 , A01N43/90 , C07D487/00
CPC分类号： C07D487/04
摘要： The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
摘要翻译：本申请描述了根据式I和II的化合物，包含至少一种式I或II的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I和II的化合物的治疗方法单独并与一种或多种另外的治疗剂组合。该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 3，本文描述了R 4和R 5。

6. 发明授权

US07378418B2 Azabicyclic heterocycles as cannabinoid receptor modulators 有权
标题翻译：氮杂环杂环作为大麻素受体调节剂
公开(公告)号：US07378418B2
公开(公告)日：2008-05-27
申请号：US11016135
申请日：2004-12-17
申请人： Guixue Yu , William R. Ewing , Amarendra B. Mikkilineni , Annapurna Pendri , Philip M. Sher , Samuel Gerritz , Bruce A. Ellsworth , Gang Wu , Yanting Huang , Chongqing Sun , Natesan Murugesan , Zhengxiang Gu , Ying Wang , Doree Sitkoff , Stephen R. Johnson , Ximao Wu
发明人： Guixue Yu , William R. Ewing , Amarendra B. Mikkilineni , Annapurna Pendri , Philip M. Sher , Samuel Gerritz , Bruce A. Ellsworth , Gang Wu , Yanting Huang , Chongqing Sun , Natesan Murugesan , Zhengxiang Gu , Ying Wang , Doree Sitkoff , Stephen R. Johnson , Ximao Wu
IPC分类号： C07D487/04 , A61K31/4162 , A61P3/04 , A61P43/00
CPC分类号： C07D487/04
摘要： The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R6, R7, m and n are described herein.
摘要翻译：本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的治疗剂。该化合物具有通式I：包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 3，本文描述了SUP 6，R 7，m和n。

7. 发明授权

US07098235B2 Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds 有权
标题翻译：甘油三酸酯和甘油三酸酯类前体药物的糖原磷酸化酶抑制化合物
公开(公告)号：US07098235B2
公开(公告)日：2006-08-29
申请号：US10712823
申请日：2003-11-13
申请人： Philip M. Sher , Bruce A. Ellsworth
发明人： Philip M. Sher , Bruce A. Ellsworth
IPC分类号： C07D209/04 , A01N43/38
CPC分类号： C07K5/0827 , A61K31/496 , A61K45/06 , C07K5/06139 , C07K5/06191 , C07K5/0821 , A61K2300/00
摘要： Prodrugs of glycogen phosphorylase inhibiting compounds are provided which are useful in treating diabetes, having the formula I G(—O2CR′)m(—OH)n(—O2C(CH2)pCH3)qI wherein G is a C3 to C5 branched or straight carbon chain and (—O2CR′), (—OH) and (—O2C(CH2)pCH3) are attached to any available carbon atom along G; —O2CR′ is a fragment of a compound of formula Ib where W is a bicyclic heteroaryl; m, n, p, q, X, Y, Z, R1 and R2 are as defined herein, as exemplified by Further provided are pharmaceutical compositions and methods for treating diabetes and related diseases employing the above compounds above, either alone or in combination with another therapeutic agent.
摘要翻译：提供了可用于治疗糖尿病的糖原磷酸化酶抑制化合物的前药，其具有式I <？in-line-formula description =“In-line Formulas”end =“lead”？> G（-O < （ - OH）n - （ - O 2 C（CH 2））其中G（x，y，y，y）是C 5 -C 5支链或直链碳链和（-O 2 R 2 CR'），（-OH）和（-O 沿着G连接到任何可用的碳原子上; C 1 -C 3烷基（CH 2 CH 2 CH 2 CH 2 CH 2） -O 2 CR'是其中W是双环杂芳基的式Ib化合物的片段; m，n，p，q，X，Y，Z，R 1和R 2均如本文所定义，作为示例。进一步提供的是药物组合物和治疗方法使用上述化合物的糖尿病和相关疾病，单独或与另一种治疗剂组合。

8. 发明授权

US5491134A Sulfonic, phosphonic or phosphiniic acid .beta..sub.3 agonist derivatives 失效
标题翻译：磺酸，膦酸或次膦酸β3激动剂衍生物
公开(公告)号：US5491134A
公开(公告)日：1996-02-13
申请号：US307217
申请日：1994-09-16
申请人： Philip M. Sher , Arvind Mathur
发明人： Philip M. Sher , Arvind Mathur
IPC分类号： C07C309/11 , C07F9/38 , C07F9/40 , A61K31/66 , A61K31/185 , C07F9/30
CPC分类号： C07F9/3808 , C07C309/11 , C07F9/4006
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: A is a bond or --OCH.sub.2 --, where the oxygen is linked to R.sup.1 ;B is --CH.sub.2 -- or when R.sup.3 is hydrogen, B may be --CH.sub.2 O-- where the oxygen is linked to the phenyl ring;R.sup.1 is an aryl group;R.sup.2 is hydrogen or lower alkyl;R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 together form the group --CH.sub.2 CH.sub.2 --; andR.sup.4 is --SO.sub.3 H, --P(O.sub.2 H)R.sup.5, --P(O.sub.2 R.sup.5')R.sup.5, --PO.sub.3 H.sub.2, --PO.sub.3 HR.sup.5' or --PO.sub.3 (R.sup.5').sub.2 where R.sup.5 and R.sup.5' are independently lower alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, for example, in the treatment of diabetes, obesity, achalasia, and gastrointestinal diseases.
摘要翻译：式Ⅰ化合物及其药学上可接受的盐，其中：A是一个键或-OCH 2 - ，其中氧连接到R 1; B是-CH 2 - 或当R 3是氢时，B可以是-CH 2 O-，其中氧连接到苯环上; R1是芳基; R2是氢或低级烷基; R3是氢; 或R 2和R 3一起形成基团-CH 2 CH 2 - ; R4是-SO3H，-P（O2H）R5，-P（O2R5'）R5，-PO3H2，-PO3HR5'或-PO3（R5'）2，其中R5和R5'独立地是低级烷基。这些化合物是β3肾上腺素能受体激动剂，并且可用于例如治疗糖尿病，肥胖症，贲门失弛缓症和胃肠道疾病。

9. 发明授权

US5153327A 7-Oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
标题翻译：可用于治疗血栓形成和血管痉挛性疾病的7-氧杂双环庚基取代的杂环酰胺或酯前列腺素类似物
公开(公告)号：US5153327A
公开(公告)日：1992-10-06
申请号：US774424
申请日：1991-10-10
申请人： Raj N. Misra , Philip M. Sher , Philip D. Stein , Steven E. Hall , David Floyd , Joel C. Barrish
发明人： Raj N. Misra , Philip M. Sher , Philip D. Stein , Steven E. Hall , David Floyd , Joel C. Barrish
IPC分类号： C07C17/16 , C07C45/29 , C07D493/08
CPC分类号： C07D493/08 , C07C17/16 , C07C45/29
摘要： 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is ##STR3## then Y cannot be O, and when Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3 m CONHR.sup.3a or --CH.sub.2 -5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.
摘要翻译：可用于治疗血栓形成和血管痉挛性疾病的7-氧杂双环庚烷取代的前列腺素类似物具有结构式：其中m为1,2或3; n为1,2,3或4; Z为 - （CH 2）2 - ， - CH = CH-或其中Y为O，单键或乙烯基，条件是当n为O时，如果Z为“IMAGE”，则Y不能为O，当Z为-CH = CH-时，n为1,2,3或4; 当Y =乙烯基时，n = R是CO 2 H，CO 2低级烷基，CH 2 OH，CO 2碱金属，CONHSOR 3 m CONHR 3 a或-CH 2 5-四唑基，X是O，S或NH; 并且其中R 1，R 2，R 3和R 3a如本文所定义。

10. 发明授权

US4975452A Geminally substituted thiaheterocyclic carboxylic acids and derivatives thereof 失效
标题翻译：金取代的噻唑烷羧酸及其衍生物
公开(公告)号：US4975452A
公开(公告)日：1990-12-04
申请号：US361620
申请日：1989-06-02
申请人： Philip M. Sher , Steven E. Hall
发明人： Philip M. Sher , Steven E. Hall
IPC分类号： A61K31/38 , A61K31/381 , A61K31/425 , A61K45/00 , A61P3/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/08 , A61P13/02 , A61P15/00 , A61P17/00 , A61P43/00 , C07D275/02 , C07D333/48 , C07F7/18
CPC分类号： C07D275/02 , C07D333/48
摘要： Novel thromboxane receptor antagonists are disclosed, having the formula ##STR1## wherein: A is aryl, optionally substituted withhalogen,lower alkoxy,carboalkoxy,lower alkyl,alkylamino, orphenyl;X is --CH.sub.2 or --NH;R.sub.1 is COOH, COO-alkali metal (such as Na, K, or Li), COO-lower alkyl, CONHSO.sub.2 R.sub.2, or 5-tetrazolyl;R.sub.2 is lower alkyl or aryl;m is 0, 1, or 2; andp is 2, 3, 4 or 5.Also disclosed are novel intermediates of formula I compounds.

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