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1. 发明授权

US08748596B2 Process for the preparation of histamine H3 receptor modulators 有权
标题翻译：组胺H3受体调节剂的制备方法
公开(公告)号：US08748596B2
公开(公告)日：2014-06-10
申请号：US13257224
申请日：2010-03-17
申请人： Diego Broggini , Vit Lellek , Susanne Lochner , Neelakandha S. Mani , Adrian Maurer , Daniel J. Pippel , Lana K. Young
发明人： Diego Broggini , Vit Lellek , Susanne Lochner , Neelakandha S. Mani , Adrian Maurer , Daniel J. Pippel , Lana K. Young
IPC分类号： C07D401/02 , C07D401/14
CPC分类号： C07D213/82 , C07B2200/13 , C07D405/12
摘要： The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.
摘要翻译：本发明涉及用于制备组胺H3受体调节剂在治疗例如认知障碍，睡眠障碍和/或精神疾病中的新方法。

2. 发明授权

US08071782B2 Synthesis of 1,3,4-trisubstituted and 1,3,4,5-tetrasubstituted pyrazoles 有权
标题翻译： 1,3,4-三取代和1,3,4,5-四取代的吡唑的合成
公开(公告)号：US08071782B2
公开(公告)日：2011-12-06
申请号：US12244184
申请日：2008-10-02
申请人： Xiaohu Deng , Neelakandha S. Mani
发明人： Xiaohu Deng , Neelakandha S. Mani
IPC分类号： C07D401/02 , C07D231/56 , C07D231/10
CPC分类号： C07D213/77 , C07D231/12 , C07D231/38 , C07D231/56 , C07D401/04 , C07D405/04 , C07D409/04
摘要： This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.
摘要翻译：本发明涉及通过腙与硝基烯烃的反应来合成高度取代的吡唑，它是药物化合物的结构组分。

3. 发明授权

US08063206B2 Processes for the preparation of cyclopropyl-amide derivatives 有权
标题翻译：制备环丙基 - 酰胺衍生物的方法
公开(公告)号：US08063206B2
公开(公告)日：2011-11-22
申请号：US12840134
申请日：2010-07-20
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
摘要翻译：本发明涉及用于制备环丙基 - 酰胺衍生物的新方法，其用于治疗由组胺受体介导的病症和病症。

4. 发明申请

US20110190503A1 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 审中-公开
标题翻译：噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯胺作为白三烯A4水解酶的调节剂
公开(公告)号：US20110190503A1
公开(公告)日：2011-08-04
申请号：US13039105
申请日：2011-03-02
申请人： Genesis M. BACANI , Diego BROGGINI , Eugene Y. CHEUNG , Christa C. CHROVIAN , Xiaohu DENG , Anne M. FOURIE , Laurent GOMEZ , Cheryl A. GRICE , Aaron M. KEARNEY , Adrienne M. LANDRY-BAYLE , Alice LEE-DUTRA , Jimmy T. LIANG , Susanne LOCHNER , Neelakandha S. MANI , Alejandro SANTILLÁN, JR. , Kathleen SAPPEY , Kia SEPASSI , Virginia M. TANIS , Alvah T. WICKBOLDT , John J. M. WIENER , Hartmut ZINSER
发明人： Genesis M. BACANI , Diego BROGGINI , Eugene Y. CHEUNG , Christa C. CHROVIAN , Xiaohu DENG , Anne M. FOURIE , Laurent GOMEZ , Cheryl A. GRICE , Aaron M. KEARNEY , Adrienne M. LANDRY-BAYLE , Alice LEE-DUTRA , Jimmy T. LIANG , Susanne LOCHNER , Neelakandha S. MANI , Alejandro SANTILLÁN, JR. , Kathleen SAPPEY , Kia SEPASSI , Virginia M. TANIS , Alvah T. WICKBOLDT , John J. M. WIENER , Hartmut ZINSER
IPC分类号： C07D451/02
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

5. 发明申请

US20100286391A1 NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES 有权
标题翻译：制备环丙基酰胺衍生物的新方法
公开(公告)号：US20100286391A1
公开(公告)日：2010-11-11
申请号：US12840134
申请日：2010-07-20
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10 , C07D401/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
摘要翻译：本发明涉及用于制备环丙基 - 酰胺衍生物的新方法，其用于治疗由组胺受体介导的病症和病症。

6. 发明授权

US07777031B2 Substituted pyridyl amide compounds as modulators of the histamine H3 receptor 有权
标题翻译：取代的吡啶酰胺化合物作为组胺H3受体的调节剂
公开(公告)号：US07777031B2
公开(公告)日：2010-08-17
申请号：US11753607
申请日：2007-05-25
申请人： Neelakandha S. Mani , John E. Mills , Chennagiri R. Pandit , Frank J. Villani , Hua Zhong
发明人： Neelakandha S. Mani , John E. Mills , Chennagiri R. Pandit , Frank J. Villani , Hua Zhong
IPC分类号： C07D243/00
CPC分类号： C07D213/82 , C07D213/81 , C07D213/84 , C07D401/06
摘要： Processes are disclosed for making certain compounds of Formula (II): or their pharmaceutically active salts, that are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases. In one embodiment, the process comprises reacting a compound of formula (7-1): with a compound of formula (B3): in the presence of at least one equivalent of a first base, in a first organic solvent, to give a compound of Formula (II).
摘要翻译：公开了制备某些式（II）化合物或其药学活性盐的方法，即组胺H3受体调节剂可用于治疗组胺H3受体介导的疾病。在一个实施方案中，该方法包括使式（7-1）化合物与式（B3）化合物在至少一当量的第一碱的存在下在第一有机溶剂中反应，得到化合物的式（II）。

7. 发明申请

US20090291903A1 SUBSTITUTED PYRROLIDINE AMIDES AS MODULATORS OF THE HISTAMINE H3 RECEPTOR 有权
标题翻译：作为组胺H3受体的调节剂的替代吡咯烷
公开(公告)号：US20090291903A1
公开(公告)日：2009-11-26
申请号：US12468632
申请日：2009-05-19
申请人： Nicholas I. Carruthers , Michael A. Letavic , Kiev S. Ly , Neelakandha S. Mani , Daniel J. Pippel , Chandravadan R. Shah , Akinola Soyode-Johnson , Emily M. Stocking , Lana Young
发明人： Nicholas I. Carruthers , Michael A. Letavic , Kiev S. Ly , Neelakandha S. Mani , Daniel J. Pippel , Chandravadan R. Shah , Akinola Soyode-Johnson , Emily M. Stocking , Lana Young
IPC分类号： A61K38/05 , C07D403/06 , A61K31/551
CPC分类号： C07D403/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Certain substituted pyrrolidine amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
摘要翻译：某些取代的吡咯烷酰胺化合物是可用于治疗组胺H3受体介导的疾病的组胺H3受体调节剂。

8. 发明申请

US20090258854A1 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 有权
标题翻译：噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯胺作为白三烯A4水解酶的调节剂
公开(公告)号：US20090258854A1
公开(公告)日：2009-10-15
申请号：US12421406
申请日：2009-04-09
申请人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearny , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillan, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
发明人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearny , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillan, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
IPC分类号： A61K31/437 , C07D513/04 , A61K31/506 , A61K31/5377 , A61K31/4985 , A61P29/00 , C12N9/50 , C07D453/02
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

9. 发明申请

US20080194577A1 2-Aminopyrimidine modulators of the histamine H4 receptor 有权
标题翻译：组胺H 4受体的2-氨基嘧啶调节剂
公开(公告)号：US20080194577A1
公开(公告)日：2008-08-14
申请号：US12070051
申请日：2008-02-14
申请人： Hui Cai , Frank Chavez , James P. Edwards , Anne E. Fitzgerald , Jing Liu , Neelakandha S. Mani , Danielle K. Neff , Michele C. Rizzolio , Brad M. Savall , Deborah M. Smith , Jennifer D. Venable , Jianmei Wei , Ronald L. Wolin
发明人： Hui Cai , Frank Chavez , James P. Edwards , Anne E. Fitzgerald , Jing Liu , Neelakandha S. Mani , Danielle K. Neff , Michele C. Rizzolio , Brad M. Savall , Deborah M. Smith , Jennifer D. Venable , Jianmei Wei , Ronald L. Wolin
IPC分类号： A61K31/496 , C07D239/48 , A61K31/505 , A61P37/08 , C07K14/705 , A61P17/00 , A61P29/00 , C07D403/04
CPC分类号： C07D498/04 , C07D239/48 , C07D239/70 , C07D239/95 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/10 , C07D519/00
摘要： 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
摘要翻译：描述了2-氨基嘧啶化合物，其可用作H 4 S 5受体调节剂。这样的化合物可以用于治疗由H 4 S受体活性介导的疾病状态，病症和病症的药物组合物和方法，例如过敏，哮喘，自身免疫疾病和瘙痒症。

10. 发明授权

US5981575A Inhibition of fatty acid synthase as a means to reduce adipocyte mass 失效
标题翻译：抑制脂肪酸合酶作为减少脂肪细胞质量的手段
公开(公告)号：US5981575A
公开(公告)日：1999-11-09
申请号：US157
申请日：1998-01-27
申请人： Francis P. Kuhajda , Gary R. Pasternack , Craig A. Townsend , Neelakandha S. Mani
发明人： Francis P. Kuhajda , Gary R. Pasternack , Craig A. Townsend , Neelakandha S. Mani
IPC分类号： A61K31/00 , A61K31/365 , A61K31/381 , A61K31/4025 , A01K31/04
CPC分类号： A61K31/4025 , A61K31/00 , A61K31/365 , A61K31/381
摘要： Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-esteem improvement, weight loss via reduction of adipocyte mass may: (1) ameliorate hyperglycemia associated with non-insulin-dependent diabetes mellitus thereby reducing diabetic complications such as arterial disease, blindness, cataracts, etc., (2) reduce hypertension, (3) reduce risk of coronary artery vascular disease and stroke, and (4) reduce the risk of other complications of massive obesity such as osteoarthritis, surgical complications, etc. There is also potential use in livestock and poultry to reduce the saturated fat content of meat products. Therefore FAS inhibitors are disclosed herein as novel agents for weight reduction. A family of compounds (.gamma.-substituted-.alpha.-methylene-.beta.-carboxy-.gamma.-butyrolactones) whose synthesis was based on the cerulenin motif is shown herein to inhibit fatty acid synthesis, inhibit growth in certain susceptible tumor cells, and induce weight loss.
摘要翻译： PCT No.PCT / US96 / 17678 Sec。 371日期：1998年1月27日 102（e）日期1998年1月27日PCT 1996年11月15日PCT PCT。第WO97 / 18806号公报日期1997年5月29日在使用非竞争性FAS抑制剂的木瓜素治疗的裸小鼠中观察到重度损失。持续减少人体脂肪细胞质量无毒性将严重影响全球疾病预防。除了心理和自尊心的改善之外，通过减少脂肪细胞质量可以减轻体重：（1）改善与非胰岛素依赖性糖尿病相关的高血糖，从而减少糖尿病并发症，如动脉疾病，失明，白内障等（2 ）降低高血压，（3）降低冠状动脉血管疾病和中风的风险，（4）降低骨质疏松，手术并发症等巨大肥胖的其他并发症的风险。畜禽养殖也有可能减少肉制品的饱和脂肪含量。因此，本文公开了FAS抑制剂作为减轻体重的新型药剂。本文显示了其合成基于苏氨酸基序的化合物（γ-取代-α-亚甲基-β-羧基-γ-丁内酯）家族，以抑制脂肪酸合成，抑制某些易感的肿瘤细胞中的生长，并诱导体重减轻。

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