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1. 发明申请

US20120214767A1 TRICYCLIC HETEROCYCLIC COMPOUNDS 有权
标题翻译：三元杂环化合物
公开(公告)号：US20120214767A1
公开(公告)日：2012-08-23
申请号：US13504541
申请日：2010-10-29
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
IPC分类号： A61K31/423 , C07D498/04 , A61K31/454 , C07D413/04 , A61P37/00 , A61K31/5377 , C07F9/09 , A61K31/675 , A61P35/00 , A61P7/00 , C07D413/14 , A61K31/506
CPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
摘要： Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其立体异构体或其盐，其中：X1，X2，X3，W，Q1，Q2和G2在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

2. 发明申请

US20100113532A1 MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途
公开(公告)号：US20100113532A1
公开(公告)日：2010-05-06
申请号：US12631179
申请日：2009-12-04
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Bingwei Yang
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Bingwei Yang
IPC分类号： A61K31/4196 , C07D249/14 , C07D401/10 , C07D417/10 , A61K31/4439 , A61P19/02 , A61P3/10 , A61P11/06
CPC分类号： C07D401/10 , C07D249/14 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10
摘要： A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供一类新型非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）或（II）的结构：包括其立体异构体，其互变异构体，其前体药物或其药学上可接受的盐，其中Q选自N，O和S; Y是芳基或杂芳基; Z是H，C 2-6烷基，环烷基，杂环烷基，芳基，杂芳基，卤素或烷氧基; 并且A，B，R，Ra，Rb，Rc和Rd在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

3. 发明申请

US20100076014A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途
公开(公告)号：US20100076014A1
公开(公告)日：2010-03-25
申请号：US12513192
申请日：2007-10-31
申请人： James E. Sheppeck , John l. Gilmore , T.G. Murali Dhar , Hai-Yun Xiao
发明人： James E. Sheppeck , John l. Gilmore , T.G. Murali Dhar , Hai-Yun Xiao
IPC分类号： A61K31/427 , C07D417/12 , C07D417/14 , C07D401/12 , C07D471/04 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，和/或AP-1和/或NF-κB活性相关的疾病，包括炎性和免疫疾病，肥胖症和糖尿病，其结构为式（I），其对映异构体，非对映体或其药学上可接受的盐或水合物，其中（Ia）是杂环或杂芳基; J，Ja，E，F，G，Ma，M，Q，Za和Z如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病和肥胖症和糖尿病的药物组合物和方法。

4. 发明申请

US20110263494A1 NONSTEROIDAL COMPOUNDS USEFUL AS MODULATORS OF GLUCOCORTICOID RECEPTOR AP-1 AND/OR NF-KAPPAB ACITIVITY AND USE THEREOF 有权
标题翻译：作为葡萄糖激动素受体AP-1和/或NF-KAPPAB活性的调节剂的非甾体化合物和其用途
公开(公告)号：US20110263494A1
公开(公告)日：2011-10-27
申请号：US12741597
申请日：2008-10-30
申请人： T.G. Murali Dhar , Hai-Yun Xiao
发明人： T.G. Murali Dhar , Hai-Yun Xiao
IPC分类号： A61K38/28 , C07D491/20 , A61K31/437 , A61K31/506 , A61K38/26 , A61P3/10 , A61P3/04 , A61P29/00 , A61P37/06 , A61P19/02 , A61P25/28 , A61P11/06 , A61P1/00 , A61P17/00 , A61P17/06 , A61P17/08 , A61P11/00 , A61P27/02 , A61P1/16 , A61P9/10 , A61P7/06 , A61P13/12 , A61P3/00 , A61P11/02 , A61P27/14 , A61P35/00 , A61P35/02 , C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are compounds of Formula (I) wherein: one of A and D is —N— and the other of A and D is —C—; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.
摘要翻译：公开了式（I）的化合物，其中：A和D之一是-N-，A和D中的另一个是-C-; 或其对映异构体，非对映异构体或其药学上可接受的盐。还公开了使用这些化合物调节糖皮质激素受体活性的功能的方法和包含这些化合物的药物组合物。

5. 发明申请

US20120202802A1 SPIROCYCLIC COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：作为化合物受体活性调节剂的螺旋化合物
公开(公告)号：US20120202802A1
公开(公告)日：2012-08-09
申请号：US13500323
申请日：2010-10-06
申请人： T.G. Murali Dhar , John V. Duncia , Daniel S. Gardner , Weiwei Guo , John Hynes
发明人： T.G. Murali Dhar , John V. Duncia , Daniel S. Gardner , Weiwei Guo , John Hynes
IPC分类号： A61K31/537 , C07D401/12 , A61K31/527 , A61K31/454 , C07D471/10 , A61K31/4545 , A61K31/4523 , A61P1/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P9/00 , A61P31/18 , A61P17/06 , A61P11/00 , A61P13/12 , A61P11/06 , A61P9/10 , A61P35/00 , C07D405/12 , C07D413/12
CPC分类号： C07D471/10 , A61K31/4427 , C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的趋化因子受体活性的调节剂或其立体异构体或其药学上可接受的盐。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和移植排斥反应的自身免疫病态的方法。

6. 发明授权

US08410139B2 Prodrugs of a piperidinyl derivative as modulators of chemokine receptor activity 有权
标题翻译：哌啶衍生物的前药作为趋化因子受体活性的调节剂
公开(公告)号：US08410139B2
公开(公告)日：2013-04-02
申请号：US12896955
申请日：2010-10-04
申请人： John Hynes , Percy H. Carter , Lyndon A. M. Cornelius , T.G. Murali Dhar , John V. Duncia , Satheesh Nair , Joseph B. Santella , Jayakumar S. Warrier , Hong Wu
发明人： John Hynes , Percy H. Carter , Lyndon A. M. Cornelius , T.G. Murali Dhar , John V. Duncia , Satheesh Nair , Joseph B. Santella , Jayakumar S. Warrier , Hong Wu
IPC分类号： A61K31/445 , C07D211/44
CPC分类号： C07D211/60 , C07D211/52 , C07F9/59
摘要： The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
摘要翻译：本申请描述了式（I）化合物的前药或其立体异构体或其药学上可接受的盐。此外，公开了使用本发明的前药化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫性病症如类风湿性关节炎的方法。

7. 发明申请

US20100204274A1 PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：作为化合物受体活性调节剂的哌啶衍生物
公开(公告)号：US20100204274A1
公开(公告)日：2010-08-12
申请号：US12670016
申请日：2008-07-23
申请人： Daniel S. Gardner , John V. Duncia , John Hynes , T.G. Murali Dhar , Percy H. Carter , Joseph B. Santella
发明人： Daniel S. Gardner , John V. Duncia , John Hynes , T.G. Murali Dhar , Percy H. Carter , Joseph B. Santella
IPC分类号： A61K31/4545 , C07D401/12 , A61K31/454 , C07D211/94 , A61K31/451 , C07D405/06 , C07D213/89 , A61P19/00 , A61P29/00 , A61P37/00
CPC分类号： C07D401/12 , C07D211/52 , C07D405/12
摘要： The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的MIP-1α或其立体异构体或前药或其药学上可接受的盐的调节剂，其中m，Q，T，W，Z，R 1，R 3，R 4，R 5，R 5a和R 5b如上定义这里。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和动脉粥样硬化的自身免疫病态的方法。

8. 发明申请

US20080275052A1 HETEROBICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
标题翻译：有机化合物作为激酶抑制剂有用
公开(公告)号：US20080275052A1
公开(公告)日：2008-11-06
申请号：US11940382
申请日：2007-11-15
申请人： T.G. Murali Dhar , Stephen T. Wrobleski
发明人： T.G. Murali Dhar , Stephen T. Wrobleski
IPC分类号： A61K31/4985 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61P11/06 , A61P9/00 , A61P3/10 , A61P1/00 , A61P17/06 , A61P9/10
CPC分类号： C07D487/04
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐。还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

9. 发明申请

US20080269499A1 CRYSTALLINE FORMS AND PROCESS FOR PREPARING SPIRO-HYDANTOIN COMPOUNDS 审中-公开
标题翻译：晶体形式和制备SPIRO-HYDANTOIN化合物的方法
公开(公告)号：US20080269499A1
公开(公告)日：2008-10-30
申请号：US12130915
申请日：2008-05-30
申请人： Albert J. DelMonte , T.G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
发明人： Albert J. DelMonte , T.G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.
摘要翻译：提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及使用它。提供某些中间体的结晶形式。

10. 发明申请

US20100063051A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途
公开(公告)号：US20100063051A1
公开(公告)日：2010-03-11
申请号：US12513187
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
发明人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
IPC分类号： A61K31/5377 , C07D277/38 , C07D417/12 , A61K31/426 , A61P37/00 , A61P29/00
CPC分类号： C07D211/58 , C07C235/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/10 , C07D417/12
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

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