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71. 发明授权

US07408066B2 Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
标题翻译：碳链取代的哌啶及其衍生物可用作组胺H3拮抗剂
公开(公告)号：US07408066B2
公开(公告)日：2008-08-05
申请号：US11455873
申请日：2006-06-19
申请人： Robert G. Aslanian , Michael Y. Berlin , Ying Huang , Kevin D. McCormick , Mwangi W. Mutahi , Neng-Yang Shih , Pauline C. Ting , Wing C. Tom , Junying Zheng
发明人： Robert G. Aslanian , Michael Y. Berlin , Ying Huang , Kevin D. McCormick , Mwangi W. Mutahi , Neng-Yang Shih , Pauline C. Ting , Wing C. Tom , Junying Zheng
IPC分类号： C07D401/04 , C07D401/14 , A61K31/495
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： Disclosed are 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, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders 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，其中：M 1和M 3是CH或N; M 2是CH，CF或N; Y是-C（-O） - ， - C（-S） - ， - （CH 2 CH 2）q - ， - C（-NOR 7） / SO 2 - ） - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H，烷基，烯基或任选取代的环烷基，芳基，杂芳基，杂环烷基或下式的基团：其中环A是单杂芳基环; 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; 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，代谢综合征非酒精性脂肪性肝病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌或认知缺陷障碍的组合物和方法。

72. 发明授权

US07531660B2 1-[[1-[(2-amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-B]pyridin-3-YL]piperidine and methods of use thereof 失效
标题翻译： 1 - [[1 - [（2-氨基-6-甲基-4-吡啶基）甲基] -4-氟-4-哌啶基]羰基] -4- [2-（2-吡啶基）-3H-咪唑并[4 ，5-B]吡啶-3-YL]哌啶及其使用方法
公开(公告)号：US07531660B2
公开(公告)日：2009-05-12
申请号：US11837248
申请日：2007-08-10
申请人： Manuel de Lera Ruiz , Robert G. Aslanian , Michael Y. Berlin , Kevin D. McCormick , Chander S. Celly
发明人： Manuel de Lera Ruiz , Robert G. Aslanian , Michael Y. Berlin , Kevin D. McCormick , Chander S. Celly
IPC分类号： C07D498/02 , A01N43/42
CPC分类号： C07D471/04
摘要： The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
摘要翻译：本发明公开了式I化合物及其药学上可接受的盐和溶剂化物。本发明还涉及包含式I化合物及其在治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病中的用途的药物组合物。本发明还涉及式I化合物与用于治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病的其它治疗剂的组合的用途。

73. 发明授权

US07332604B2 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine 失效
标题翻译： 1 - [[1 - [（2-氨基-6-甲基-4-吡啶基）甲基] -4-氟-4-哌啶基]羰基] -4- [2-（2-吡啶基）-3H-咪唑并[4 ，5-b]吡啶-3-基]哌啶
公开(公告)号：US07332604B2
公开(公告)日：2008-02-19
申请号：US11523489
申请日：2006-09-19
申请人： Manuel de Lera Ruiz , Robert G. Aslanian , Michael Y. Berlin , Kevin D. McCormick
发明人： Manuel de Lera Ruiz , Robert G. Aslanian , Michael Y. Berlin , Kevin D. McCormick
IPC分类号： C07D498/02
CPC分类号： C07D471/04
摘要： The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
摘要翻译：本发明公开了式I化合物及其药学上可接受的盐和溶剂化物。本发明还涉及包含式I化合物及其在治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病中的用途的药物组合物。本发明还涉及式I化合物与用于治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病的其它治疗剂的组合的用途。

74. 发明授权

US06762186B2 Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists 失效
标题翻译：取代的咪唑作为双组胺H1和H3激动剂或拮抗剂
公开(公告)号：US06762186B2
公开(公告)日：2004-07-13
申请号：US09955383
申请日：2001-09-18
申请人： Neng-Yang Shih , Robert G. Aslanian , Daniel M. Solomon , Stuart B. Rosenblum , Mwangi Wa Mutahi , Tom G. Wing , Kevin D. McCormick , John J. Piwinski , Ronald Wolin
发明人： Neng-Yang Shih , Robert G. Aslanian , Daniel M. Solomon , Stuart B. Rosenblum , Mwangi Wa Mutahi , Tom G. Wing , Kevin D. McCormick , John J. Piwinski , Ronald Wolin
IPC分类号： C07D21168
CPC分类号： C07D233/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06
摘要： The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, nasal congestion, inflammatory and CNS-related diseases and others.
摘要翻译：本发明公开了具有H3受体拮抗剂或双组胺H1和H3受体拮抗剂活性的新型取代咪唑化合物以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含这种咪唑的药物组合物以及使用它们治疗过敏，鼻充血，炎性和CNS相关疾病等的方法。

75. 发明授权

US5696267A Substituted oximes, hydrazones and olefins as neurokinin antagonists 失效
标题翻译：取代的肟，腙和烯烃作为神经激肽拮抗剂
公开(公告)号：US5696267A
公开(公告)日：1997-12-09
申请号：US641384
申请日：1996-04-30
申请人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
发明人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D295/185 , C07D333/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/04 , C07D211/08
CPC分类号： C07D295/185 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D333/22 , C07D401/04 , C07D401/06 , C07D409/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3;b, d and e are independently 0, 1 or 2; R is H, C.sub.1-6 alkyl, --OH or C.sub.2 -C.sub.6 hydroxyalkyl; A is an optionally substituted oxime, hydrazone or olefin; X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)--OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.1)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --,--N(R.sup.6)C(O)O-- or --OC(O)--; T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6, phenyl, naphthyl or heteroaryl; R.sup.6a, R.sup.7a, R.sup.8a, R.sup.9a, R.sup.6 and R.sup.7 are H, C.sub.1-6 alkyl, C.sub.2 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; or R.sup.6 and R.sup.7, together with the nitrogen to which they are attached, form a ring; R.sup.9a is R.sup.6 or --OR.sup.6 ; Z is morpholinyl, optionally N-substituted piperazinyl, optionally substituted ##STR2## or substituted ##STR3## g is 0-3 and h is 1-4, provided the sum of h and g is 1-7; wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式I表示的化合物或其药学上可接受的盐，其中：a为0,1,2或3; b，d和e独立地为0,1或2; R为H，C 1-6烷基，-OH或C 2 -C 6羟基烷基; A是任选取代的肟，腙或烯烃; X是键，-C（O） - ， - O - ， - NR6 - ， - S（O）e - ， - N（R6）C（O） - ， - （O）NR6-， - OC（= S）NR6-，-N（R6）C（= S）O-，-C（= NOR1） - ， - S（O） R6）S（O）2 - ， - N（R6）C（O）O-或-OC（O） - ; T是H，苯偶酰亚氨基，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; Q是-SR 6，-N（R 6）（R 7），-OR 6，苯基，萘基或杂芳基; R6a，R7a，R8a，R9a，R6和R7是H，C1-6烷基，C2-C6羟基烷基，C1-C6烷氧基-C1-C6烷基，苯基或苄基; 或R 6和R 7与它们所连接的氮一起形成环; R9a为R6或-OR6; Z是吗啉基，任选取代的哌嗪基，任选取代的取代的或取代的，如果h和g之和为1-7，则g是0-3，h是1-4; 其中芳基，杂环烷基，杂芳基，环烷基和桥连环烷基任选被取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，炎性疾病和胃肠道疾病的方法，以及包含所述化合物的药物组合物。

76. 发明申请

US20120172369A1 INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE 审中-公开
标题翻译：二乙酰胆碱酯酶抑制剂
公开(公告)号：US20120172369A1
公开(公告)日：2012-07-05
申请号：US13395589
申请日：2010-09-03
申请人： Pauline C. Ting , Joe F. Lee , Robert G. Aslanian
发明人： Pauline C. Ting , Joe F. Lee , Robert G. Aslanian
IPC分类号： A61K31/506 , C07D409/14 , C07D405/12 , A61K31/496 , A61P3/06 , A61K31/443 , A61K31/444 , A61K31/4525 , A61P3/04 , A61P3/10 , C07D405/14 , A61K31/4545
CPC分类号： C07D405/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:
摘要翻译：本发明涉及作为二酰基甘油酰基转移酶（DGAT）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关病症，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。本发明的说明性化合物如下所示：

77. 发明申请

US20100093692A1 PIPERIDINYL-PIPERIDINE AND PIPERAZINYL-PIPERIDINE FOR USE IN THE TREATMENT OF DIABETES OR PAIN 审中-公开
标题翻译：用于治疗糖尿病或疼痛的哌啶二哌啶和哌嗪哌啶
公开(公告)号：US20100093692A1
公开(公告)日：2010-04-15
申请号：US12527499
申请日：2008-02-27
申请人： Robert G. Aslanian , Jean E. Lachowicz , Michael Y. Berlin , Joyce J. Hwa
发明人： Robert G. Aslanian , Jean E. Lachowicz , Michael Y. Berlin , Joyce J. Hwa
IPC分类号： A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/397 , A61P3/10
CPC分类号： A61K31/4545 , A61K45/06 , A61K2300/00
摘要： The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.
摘要翻译：本发明涉及式（I）的化合物，包含该化合物的组合物，以及使用该化合物治疗或预防疼痛，糖尿病，糖尿病并发症，糖耐量异常（IGT）或空腹血糖受损（IFG）的方法患者。

78. 发明申请

US20110136790A1 Tricyclic Heterocyclic Derivatives and Methods of Use 审中-公开
标题翻译：三环杂环衍生物和使用方法
公开(公告)号：US20110136790A1
公开(公告)日：2011-06-09
申请号：US13054860
申请日：2009-07-21
申请人： Manuel De Lera Ruiz , MIchael Y Berlin , Junying Zheng , Robert G. Aslanian , Kenvin D. McCormick , Qingbel Zeng
发明人： Manuel De Lera Ruiz , MIchael Y Berlin , Junying Zheng , Robert G. Aslanian , Kenvin D. McCormick , Qingbel Zeng
IPC分类号： A61K31/55 , C07D417/14 , A61K31/5415 , A61K31/542 , C07D401/14 , C07D495/14 , A61K31/551 , A61P37/08 , A61P11/00 , A61P9/00 , A61P29/00 , A61P3/00 , A61P1/00 , A61P25/00
CPC分类号： C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/14
摘要： The present invention relates to novel Tricyclic Heterocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is —CH—. —C(halo)- or —N—; Y is —C(O)—, —S—. —S(O)—, —S(O)2—, —CH2— or —O—, such that Y is not —O— when an adjacent atom is N.
摘要翻译：本发明涉及新型三环杂环衍生物，包含三环杂环衍生物的药物组合物和这些化合物用于治疗或预防过敏，过敏诱导的气道反应，充血，心血管疾病，炎性疾病，胃肠道疾病，糖尿病，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 R1是式（Ia），（Ib）或（Ic）; R2是烷基，烯基，炔基，芳基，杂芳基，环烷基或杂环烷基。其中任何一个可以任选被R 11取代; M1是-CH-。 -C（卤代） - 或-N-; Y是-C（O） - ， - S - 。 -S（O） - ， - S（O）2 - ， - CH 2 - 或-O-，使得当相邻原子为N时，Y不为-O-

79. 发明授权

US06528522B2 Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists 失效
公开(公告)号：US06528522B2
公开(公告)日：2003-03-04
申请号：US09954863
申请日：2001-09-18
申请人： Neng-Yang Shih , Robert G. Aslanian , John J. Piwinski , Andrew T. Lupo, Jr. , Adriano Afonso
发明人： Neng-Yang Shih , Robert G. Aslanian , John J. Piwinski , Andrew T. Lupo, Jr. , Adriano Afonso
IPC分类号： A61K31435
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.

80. 发明授权

US5990147A H.sub.3 receptor ligands of the phenyl-alkyl-imidazoles type 失效
标题翻译：苯基 - 烷基 - 咪唑型的H3受体配体
公开(公告)号：US5990147A
公开(公告)日：1999-11-23
申请号：US186492
申请日：1998-11-05
申请人： Robert G. Aslanian
发明人： Robert G. Aslanian
IPC分类号： A61K31/4174 , C07D233/54 , C07D233/64 , A61K31/415
CPC分类号： C07D233/64 , A61K31/4174
摘要： Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## or pharmaceutically acceptable salts or solvates thereof, wherein A and R, are as defined in the specification.Also disclosed are methods of treating allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper and hypo motility of the gastrointestinal tract, hypo and hyperactivity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines, comprising administering an effective amount of a compound of formula I (or a salt or solvate thereof) to a patient in need of such treatment.Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H.sub.1 receptor antagonist.
摘要翻译：公开了下式的新型苯基 - 烷基 - 咪唑或其药学上可接受的盐或溶剂合物，其中A和R如说明书中所定义。还公开了治疗过敏，炎症，低血压，青光眼，睡眠障碍，胃肠道过度和低运动状态，中枢神经系统的低血压和多动症，阿尔茨海默病，精神分裂症，肥胖症和偏头痛的方法，包括给予有效量的式I化合物（或其盐或溶剂合物）给予需要这种治疗的患者。还公开了治疗上呼吸道过敏反应的方法，包括与组胺H1受体拮抗剂组合或混合施用式I化合物或其盐或溶剂合物。

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