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1. 发明申请

US20110182828A1 C20-C21 SUBSTITUTED GLUCOCORTICOID RECEPTOR AGONISTS 失效
标题翻译： C20-C21取代葡萄糖激素受体激动剂
公开(公告)号：US20110182828A1
公开(公告)日：2011-07-28
申请号：US12736063
申请日：2008-12-18
申请人： John C. Anthes , Kevin D. Mccormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Phillippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
发明人： John C. Anthes , Kevin D. Mccormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Phillippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号： A61K31/58 , C07J43/00 , C07J9/00 , C07J41/00 , C07J71/00 , A61K31/573 , A61P17/00 , A61P37/08 , A61P11/10 , A61P11/02 , A61P31/00 , A61P29/00 , A61P37/06 , A61P31/12 , A61P37/02 , A61P17/06 , A61P17/04 , A61P27/02
CPC分类号： C07J43/003
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译：本发明提供具有以下通式结构的式（I）化合物及其药学上可接受的盐，溶剂合物，酯，前体药物，互变异构体或异构体）：其中L，R1，R2，R3，R4，R5和 R6彼此独立地选择并如本文所定义。本发明还提供如本文定义的式II，III，IV，V和VI的化合物（和盐，溶剂合物，酯，前药，互变异构体和异构体）。还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。

2. 发明授权

US08524697B2 C20-C21 substituted glucocorticoid receptor agonists 失效
标题翻译： C20-C21取代的糖皮质激素受体激动剂
公开(公告)号：US08524697B2
公开(公告)日：2013-09-03
申请号：US12736063
申请日：2008-12-18
申请人： John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar , Phillippa H. Solomon
发明人： John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号： A01N43/00 , A61K31/33 , C07D215/00 , C07D277/62
CPC分类号： C07J43/003
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译：本发明提供具有以下通式结构的式（I）化合物及其药学上可接受的盐，溶剂合物，酯，前体药物，互变异构体或异构体）：其中L，R1，R2，R3，R4，R5和 R6彼此独立地选择并如本文所定义。本发明还提供如本文定义的式II，III，IV，V和VI的化合物（和盐，溶剂合物，酯，前药，互变异构体和异构体）。还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。

3. 发明申请

US20110262368A1 C21 THIOETHERS AS GLUCOCORTICOID RECEPTOR AGONISTS 审中-公开
标题翻译： C21三醇作为葡萄糖激素受体激动剂
公开(公告)号：US20110262368A1
公开(公告)日：2011-10-27
申请号：US12736064
申请日：2008-12-18
申请人： John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Philippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
发明人： John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Philippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号： A61K31/58 , C07J31/00 , A61K31/573 , A61P25/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P11/06 , A61P11/00 , A61P17/00 , A61P17/06 , A61P17/04 , A61P31/12 , A61P31/00 , A61P11/02 , A61P37/06 , A61P37/08 , A61P11/10 , C07J43/00
CPC分类号： C07J43/003 , C07J31/006 , C07J71/0031
摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
摘要翻译：本发明提供了具有通式（Ⅶ）的所述化合物和所述11-酮类似物的式（Ⅶ）化合物及其11-酮类似物及其可药用盐，溶剂合物，酯，前体药物，互变异构体和异构体，：其中L，R 1，R 2，R 3，R 4和R 5彼此独立地选择并如本文所定义。还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。本发明的新型化合物具有有用的药理活性，同时具有意想不到的全身活性。因此，本发明的化合物代表具有差的副作用特征的已知糖皮质激素的更安全的替代方案。

4. 发明申请

US20120171126A1 NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：新型[3,2-c]异烟肼作为葡萄糖激素受体激动剂组合物及其用途
公开(公告)号：US20120171126A1
公开(公告)日：2012-07-05
申请号：US13378893
申请日：2010-06-15
申请人： Biju J. Purakkattle , Michael Y. Berlin , Yeon-Hee Lim , Rema D. Bitar , Kevin D. McCormick , Robert G. Aslanian , Yoon Joo Lee , Junying Zheng , Ying Huang , Walter Won
发明人： Biju J. Purakkattle , Michael Y. Berlin , Yeon-Hee Lim , Rema D. Bitar , Kevin D. McCormick , Robert G. Aslanian , Yoon Joo Lee , Junying Zheng , Ying Huang , Walter Won
IPC分类号： A61K31/58 , A61K9/12 , A61P37/00 , A61P29/00 , A61P17/00 , A61P17/06 , A61P17/04 , A61P11/06 , A61P11/02 , A61P11/08 , A61P11/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61P27/02 , C07J71/00
CPC分类号： C07J71/0047 , C07J71/0063
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: Formula (I) wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas (H-A), (II-A1), (II-A2), (II-A2.1), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (VI), as described herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译：本发明提供具有以下通式结构的式（I）化合物及其药学上可接受的盐，溶剂合物，酯，前体药物，互变异构体或异构体：其中L，R1，R2，R3，R4 R 5和R 6彼此独立地选择并如本文所定义。本发明还提供式（IIa），（Ⅱ-A1），（Ⅱ-A2），（Ⅱ-A2.1），（Ⅱ-A2）的化合物（和盐，溶剂合物，酯，前体药物，互变异构体和异构体）（II-A-2.3），（II-A4），（HB），（HC），（III），（IV），（V），（VI）还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。

5. 发明授权

US07220735B2 Benzimidazolone histamine H3 antagonists 失效
标题翻译：苯并咪唑酮组胺H3拮抗剂
公开(公告)号：US07220735B2
公开(公告)日：2007-05-22
申请号：US10414943
申请日：2003-04-16
申请人： Pauline C. Ting , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Qingbei Zeng
发明人： Pauline C. Ting , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Qingbei Zeng
IPC分类号： A61K31/495
CPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
摘要翻译：公开了下式的新化合物其中R 1是苯并咪唑酮衍生物，M 1和M 2是任选取代的碳或氮，R SUP > 2 包括任选取代的芳基或杂芳基，其余变量如说明书中所定义，其余变量如说明书中所定义; 还公开了包含式I化合物的药物组合物和使用式I化合物治疗各种疾病或病症如过敏，过敏引起的气道反应和充血（例如，鼻塞）的方法，以及使用式I化合物与H 1受体拮抗剂组合治疗所述疾病或病症。

6. 发明授权

US07879880B2 Substituted aniline derivatives useful as histamine H3 antagonists 失效
标题翻译：用作组胺H3拮抗剂的取代苯胺衍生物
公开(公告)号：US07879880B2
公开(公告)日：2011-02-01
申请号：US11641153
申请日：2006-12-19
申请人： Daniel M. Solomon , Robert G. Aslanian , Michael Y. Berlin , Manuel de Lera Ruiz , Kevin D. McCormick , Mwangi W. Mutahi , Wing C. Tom
发明人： Daniel M. Solomon , Robert G. Aslanian , Michael Y. Berlin , Manuel de Lera Ruiz , Kevin D. McCormick , Mwangi W. Mutahi , Wing C. Tom
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4545 , C07D487/04 , C07D413/14 , C07D401/14 , C07D401/12
CPC分类号： C07D401/12 , C07D213/73 , C07D213/74 , C07D401/14 , C07D471/04
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(═O)—, —C(═NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(═O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(═NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐，其中M 1为M 2为N; X是一个键，任选取代的亚烷基，亚烯基，-O - ， - CH2-（R12） - ， - N（R12）CH2-，-N（R12） - ， - NHC（O） - ， - OCH2 - - 或-S（O）0-2-; 并且Y是 - （CH 2）1-2 - ， - C（= O） - ， - C（= NOR 13） - 或-SOO 2 - ; 或M1为N; M2为N或CH; X是键，亚烷基，亚烯基，-C（O） - ， - NHC（O） - ， - OC（O） - 或-S（O）1-2 - Y是 - （CH 2）1-2 - ， - C（= O） - 或-SOO 2 - ; 当M2是CH时，Y也是Y是-O-或-C（= NROR13） - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH，或一个是CH，一个是N; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症，代谢综合征和认知缺陷障碍的组合物和方法。

7. 发明授权

US07105505B2 Benzimidazole derivatives useful as histamine H3 antagonists 失效
标题翻译：可用作组胺H3拮抗剂的苯并咪唑衍生物
公开(公告)号：US07105505B2
公开(公告)日：2006-09-12
申请号：US10417391
申请日：2003-04-16
申请人： Qingbei Zeng , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Joseph A. Kozlowski , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom
发明人： Qingbei Zeng , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Joseph A. Kozlowski , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom
IPC分类号： A61K31/495
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Disclosed are novel compounds of the formula wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substituted aryl or heteroaryl; M1 and M2 are C(R3) or N; and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
摘要翻译：公开了下式的新化合物，其中R 1是任选取代的苯并咪唑基或其衍生物; R 2是任选取代的芳基或杂芳基; M 1和M 2是C（R 3）或N; 剩余的变量如规范中所定义; 还公开了包含式I化合物的药物组合物和使用式I化合物治疗各种疾病或病症如过敏，过敏引起的气道反应和充血（例如，鼻塞）的方法，以及使用式I化合物与H 1受体拮抗剂组合治疗所述疾病或病症。

8. 发明授权

US07846946B2 Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
标题翻译：杂原子取代的哌啶及其衍生物可用作组胺H3拮抗剂
公开(公告)号：US07846946B2
公开(公告)日：2010-12-07
申请号：US12507563
申请日：2009-07-22
申请人： Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Henry A. Vaccaro , Junying Zheng , Xiaohong Zhu
发明人： Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Henry A. Vaccaro , Junying Zheng , Xiaohong Zhu
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐，其中：M1和M3是CH或N; M2是CH，CF或N; Y是-C（= O） - ， - C（= S） - ， - （CH 2）q - ， - C（= NOR 7） - 或-SO 1 2- Z是键或任选取代的亚烷基或亚烯基; R 1是H或烷基，环烷基，芳基，杂芳基，杂环烷基，全部被取代，或下式的基团：其中环A是杂芳基环; R 2是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; R 3是H，-C（O）NH 2或烷基，芳基，环烷基，杂环烷基或杂芳基，全部被取代; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征，酒精性脂肪肝疾病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌和认知缺陷障碍的组合物和方法。

9. 发明授权

US07638531B2 Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists 失效
标题翻译：苯氧基哌啶及其类似物可用作组胺H3拮抗剂
公开(公告)号：US07638531B2
公开(公告)日：2009-12-29
申请号：US11641175
申请日：2006-12-19
申请人： Mwangi W. Mutahi , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Manuel de Lera Ruiz , Kevin D. McCormick , Daniel M. Solomon , Henry A. Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
发明人： Mwangi W. Mutahi , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Manuel de Lera Ruiz , Kevin D. McCormick , Daniel M. Solomon , Henry A. Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
IPC分类号： A01N43/42 , A61K31/44 , A01N43/40 , C07D471/02 , C07D491/02 , C07D498/02 , C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D471/04 , C07D213/38 , C07D213/73 , C07D277/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D473/00
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：M是CH或N; U和W各自为CH，或U和W中的一个为CH，另一个为N; X是键，亚烷基，-C（O） - ， - C（N-OR 5） - ， - C（N-OR 5）-CH（R 6） - ， - CH（R 6）-C（N-OR 5），-O - ， - OCH 2 - ， - CH 2 O-或-S（O）0-2-; Y是-O - ， - （CH 2）2 - ， - C（-O） - ， - C（-NOR 7） - 或-SOO 2 - ; Z是一个键，任选取代的被杂原子或杂环基中断的亚烷基或亚烷基; R1是任选取代的烷基，环烷基，芳基，芳烷基，杂芳基，杂环烷基或苯并咪唑基或其衍生物; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，糖尿病，肥胖，肥胖相关病症，代谢综合征和认知缺陷障碍的组合物和方法。

10. 发明授权

US07635705B2 Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
标题翻译：杂原子取代的哌啶及其衍生物可用作组胺H3拮抗剂
公开(公告)号：US07635705B2
公开(公告)日：2009-12-22
申请号：US11455625
申请日：2006-06-19
申请人： Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin D. McCormick , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Henry A. Vaccaro , Junying Zheng , Xiaohong Zhu , Mwangi W. Mutahi
发明人： Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin D. McCormick , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Henry A. Vaccaro , Junying Zheng , Xiaohong Zhu , Mwangi W. Mutahi
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐，其中：M1和M3是CH或N; M2是CH，CF或N; Y是-C（-O） - ， - C（-S） - ， - （CH 2）q - ， - C（-NOR 7） - 或-SO 1 - Z是键或任选取代的亚烷基或亚烯基; R 1是H或烷基，环烷基，芳基，杂芳基，杂环烷基，全部被取代，或下式的基团：其中环A是杂芳基环; R 2是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; R 3是H，-C（O）NH 2或烷基，芳基，环烷基，杂环烷基或杂芳基，全部被取代; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征，酒精性脂肪肝疾病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌和认知缺陷障碍的组合物和方法。

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