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1. 发明申请

US20100004245A1 AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯的一种维生素A的脱乙酰壳多糖衍生物
公开(公告)号：US20100004245A1
公开(公告)日：2010-01-07
申请号：US12440835
申请日：2007-10-18
申请人： Renata M. Oballa , Denis Deschenes , Marc Gagnon , Yves Leblanc , David Powell , Yeeman K. Ramtohul
发明人： Renata M. Oballa , Denis Deschenes , Marc Gagnon , Yves Leblanc , David Powell , Yeeman K. Ramtohul
IPC分类号： A61K31/53 , C07D401/14 , C07D403/14 , C07D417/14 , C07D413/14 , A61K31/4545 , A61K31/501 , A61K31/506
CPC分类号： C07D413/14 , C07D401/14 , C07D417/14
摘要： Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译：结构式（I）的Azacycalkalkane衍生物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

2. 发明申请

US20110301143A1 HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯A DELTA-9去饱和酶的抑制剂的杂环衍生物
公开(公告)号：US20110301143A1
公开(公告)日：2011-12-08
申请号：US13201720
申请日：2010-02-18
申请人： Elise Isabel , Nicolas Lachance , Jean-Philippe Leclerc , Serge Leger , Renata M. Oballa , David Powell , Yeeman K. Ramtohul , Patrick Roy , Geoffrey K. Tranmer , Renee Aspiotis , Lianhai Li , Evelyn Martins
发明人： Elise Isabel , Nicolas Lachance , Jean-Philippe Leclerc , Serge Leger , Renata M. Oballa , David Powell , Yeeman K. Ramtohul , Patrick Roy , Geoffrey K. Tranmer , Renee Aspiotis , Lianhai Li , Evelyn Martins
IPC分类号： A61K31/497 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/506 , A61K31/496 , A61K31/427 , A61K31/454 , A61K31/4439 , A61K31/4995 , A61K31/551 , A61P3/10 , A61P5/48 , A61P3/00 , A61P3/06 , A61P7/00 , C07D403/14
CPC分类号： C07D413/14 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/551 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D487/08
摘要： Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, C═CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
摘要翻译：结构式（I）的杂环化合物或其药学上可接受的盐，其中W是R1-取代的杂芳基，R1是被含有或含羧酸基团取代的杂芳基环，XT是N-CR5R6，C = CR5或 CR13-CR5R6，Y是键或-C（O） - ，a和b表示选自1至4的整数，Ar是任选取代的苯基或萘基，是硬脂酰辅酶A-9去饱和酶的抑制剂 SCD）杂环化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，动脉粥样硬化，肥胖，糖尿病，神经系统疾病，代谢综合征，胰岛素抵抗，癌症，肝脂肪变性和非酒精性脂肪性肝炎

3. 发明申请

US20090270434A1 AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯的一种维生素A的脱乙酰壳多糖衍生物
公开(公告)号：US20090270434A1
公开(公告)日：2009-10-29
申请号：US12498476
申请日：2009-07-07
申请人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Leger
发明人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Leger
IPC分类号： A61K31/506 , C07D401/14 , A61P3/10
CPC分类号： C07D401/14 , C07D403/14
摘要： Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译：结构式I的Azacycalkalkane衍生物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶A delta-9去饱和酶（SCD1）的选择性抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

4. 发明授权

US07582633B2 Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 失效
标题翻译：氮杂环烷烃衍生物作为硬脂酰辅酶抑制剂，δ-9去饱和酶
公开(公告)号：US07582633B2
公开(公告)日：2009-09-01
申请号：US12011309
申请日：2008-01-25
申请人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Léger
发明人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Léger
IPC分类号： C07D401/14 , C07D403/14 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/425 , A61P3/10 , A61P3/04
CPC分类号： C07D401/14 , C07D403/14
摘要： Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译：结构式I的Azacycalkalkane衍生物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶A delta-9去饱和酶（SCD1）的选择性抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

5. 发明申请

US20080182838A1 Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 失效
标题翻译：氮杂环烷烃衍生物作为硬脂酰辅酶抑制剂，δ-9去饱和酶
公开(公告)号：US20080182838A1
公开(公告)日：2008-07-31
申请号：US12011309
申请日：2008-01-25
申请人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Leger
发明人： Yves Leblanc , David Powell , Yeeman K. Ramtohul , Serge Leger
IPC分类号： A61K31/397 , C07D241/10 , A61K31/497 , A61P3/10 , A61P3/00 , A61P3/04 , C07D239/24 , A61K31/506
CPC分类号： C07D401/14 , C07D403/14
摘要： Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译：结构式I的Azacycalkalkane衍生物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶A delta-9去饱和酶（SCD1）的选择性抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

6. 发明申请

US20110021532A1 NOVEL SUBSTITUTED HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：新型替代异构化合物作为硬脂酸苄酯DE DELTA-9去饱和酶的抑制剂
公开(公告)号：US20110021532A1
公开(公告)日：2011-01-27
申请号：US12934100
申请日：2009-04-21
申请人： David Powell , Marie-Eve Lebrun , Sathesh Bhat , Yeeman K. Ramtohul
发明人： David Powell , Marie-Eve Lebrun , Sathesh Bhat , Yeeman K. Ramtohul
IPC分类号： A61K31/501 , C07D235/18 , A61K31/4184 , C07D401/02 , A61K31/4439 , C07D403/04 , A61K31/506 , C07D471/02 , A61K31/437 , A61P3/10 , A61P3/00 , A61P3/04 , A61P1/16 , A61P9/00 , A61P9/10
CPC分类号： C12N9/0083 , C07D235/18 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/10 , C07D409/10 , C07D471/04
摘要： Substituted heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I).
摘要翻译：结构式I的取代的杂芳族化合物是硬脂酰辅酶A delta-9去饱和酶的抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 2型糖尿病; 胰岛素抵抗; 高血糖症代谢综合征; 神经系统疾病; 癌症; 和肝脂肪变性。式（I）。

7. 发明申请

US20120010186A1 HETEROCYCLIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯A DELTA-9去饱和酶抑制剂的杂环化合物
公开(公告)号：US20120010186A1
公开(公告)日：2012-01-12
申请号：US13255922
申请日：2010-03-18
申请人： Nicolas Lachance , Serge Leger , Renata M. Oballa , David Powell , Geoffrey K. Tranmer , Evelyn Martins , Yves Gareau
发明人： Nicolas Lachance , Serge Leger , Renata M. Oballa , David Powell , Geoffrey K. Tranmer , Evelyn Martins , Yves Gareau
IPC分类号： A61K31/427 , C07D487/10 , C07D471/10 , A61P3/06 , A61K31/422 , A61K31/438 , A61K31/506 , A61P3/10 , C07D487/04 , A61K31/433
CPC分类号： C07D471/10 , C07D487/04 , C07D487/10
摘要： Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.
摘要翻译：结构式I的杂环化合物是硬脂酰辅酶A delta-9去饱和酶（SCD）的抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病; 动脉粥样硬化肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 癌症，肝脂肪变性; 和非酒精性脂肪性肝炎。

8. 发明申请

US20100152208A1 BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯A DELTA-9去饱和酶抑制剂的双相异构化合物
公开(公告)号：US20100152208A1
公开(公告)日：2010-06-17
申请号：US12600484
申请日：2008-05-22
申请人： Serge Leger , Denis Deschenes , Rejean Fortin , Elise Isabel , David Powell
发明人： Serge Leger , Denis Deschenes , Rejean Fortin , Elise Isabel , David Powell
IPC分类号： A61K31/519 , C07D513/04 , A61P3/10 , A61P3/06 , A61P9/10
CPC分类号： C07D513/04
摘要： Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I).
摘要翻译：结构式I的双环杂芳族化合物是硬脂酰辅酶A-9去饱和酶（SCD）的抑制剂。本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 2型糖尿病; 胰岛素抵抗; 高血糖症代谢综合征; 神经系统疾病; 癌症; 和肝脂肪变性。式（I）。

9. 发明申请

US20120094555A1 ELECTRIC MARINE PROPULSION DEVICE WITH INTEGRAL MAGNETIC GEARING 有权
标题翻译：具有整体磁力传动的电动海洋推进装置
公开(公告)号：US20120094555A1
公开(公告)日：2012-04-19
申请号：US13260428
申请日：2010-03-26
申请人： Stuart Calverley , David Powell
发明人： Stuart Calverley , David Powell
IPC分类号： B63H23/24 , H02K51/00
CPC分类号： B63H23/24 , B63H2005/1258 , B63H2021/202 , H02K7/11 , H02K51/00 , Y02T70/5236
摘要： A propulsion device for a marine vessel, the propulsion device comprising an electrical machine with integral magnetic gearing, which comprises three members, namely a first or inner rotor comprising a first plurality of permanent magnets, a second rotor in the form of a plurality of ferromagnetic pole pieces, and a stator which is associated with a plurality of 3-phase windings and to the periphery of which a plurality of second permanent magnets are fixed. The magnetic pole piece rotor is connected to a drive shaft provided with a propulsion means for providing propulsion to the marine vessel. The first or inner rotor is free to rotate about the drive shaft. The pole pieces of the second rotor are arranged to magnetically couple the permanent magnets of the first or inner rotor to the second permanent magnets on the stator.
摘要翻译：一种用于海洋船舶的推进装置，该推进装置包括具有整体磁力传动装置的电机，其包括三个构件，即包括第一多个永磁体的第一或第二转子，包括多个铁磁体形式的第二转子极片和与多个三相绕组相关联的定子，并且固定有多个第二永磁体的周边。磁极片转子连接到设置有用于向船舶提供推进的推进装置的驱动轴上。第一或内转子围绕驱动轴自由旋转。第二转子的极片布置成将第一或内转子的永磁体磁耦合到定子上的第二永磁体。

10. 发明申请

US20100105639A1 MESALAMINE SUPPOSITORY 有权
标题翻译：木脂素支架
公开(公告)号：US20100105639A1
公开(公告)日：2010-04-29
申请号：US12639645
申请日：2009-12-16
申请人： Yves Dumoulin , Carl Gauthier , David Powell , Hugues Moreau
发明人： Yves Dumoulin , Carl Gauthier , David Powell , Hugues Moreau
IPC分类号： A61K31/606 , A61P1/00
CPC分类号： A61K9/14 , A61K9/0031 , A61K9/02 , A61K31/136 , A61K31/195 , A61K31/606 , A61K47/44
摘要： The present invention relates to a mesalamine rectal suppository designed to provide improved comfort of use. One embodiment of the invention is a mesalamine rectal suppository comprising mesalamine and one or more pharmaceutically acceptable excipients, wherein the drug load of the suppository ranges from 35% to 50%. Yet another embodiment of the invention is a mesalamine rectal suppository comprising mesalamine having a tap density ranging from about 600 to about 800 g/L (as measured by USP ) and a hard fat having an ascending melting point of 32 to 35.5° C. Yet another embodiment is a mesalamine rectal suppository comprising mesalamine particles and one or more pharmaceutically acceptable excipients, where the mesalamine particles have a surface area of from about 0.1 m2/g to about 2.8 m2/g (e.g., from about 0.1 m2/g to about 1.3 m2/g). Methods of preparing and methods of treatment with mesalamine suppositories are also provided. The invention further provides a method of determining a dissolution parameter (such as dissolution rate) of a mesalamine rectal suppository, such as a 1 g mesalamine suppository, by measuring its dissolution with USP Apparatus #2 at 40° C. and a paddle rotation speed of 125 rpm in 0.2 M phosphate buffer at a pH of 7.5.
摘要翻译：本发明涉及美沙拉坦直肠栓剂，其旨在提供改善的使用舒适性。本发明的一个实施方案是美沙拉坦直肠栓剂，其包含美沙拉嗪和一种或多种药学上可接受的赋形剂，其中栓剂的药物负载范围为35％至50％。本发明的另一个实施方案是美沙拉坦直肠栓剂，其包含振荡密度范围为约600至约800g / L的美沙拉嗪（通过USP <616>测量）和具有上升熔点为32至35.5°的硬脂肪 C.另一个实施方案是美沙拉坦直肠栓剂，其包含美沙拉嗪颗粒和一种或多种药学上可接受的赋形剂，其中美沙拉嗪颗粒的表面积为约0.1m 2 / g至约2.8m 2 / g（例如，约0.1m 2 / g至约1.3m 2 / g）。还提供了制备方法和美沙拉坦栓剂的治疗方法。本发明还提供了一种通过用USP装置＃2在40℃下测量溶解参数（例如溶解度）来测定美沙拉嗪直肠栓剂如1g美沙胺栓剂的溶出参数（如溶出速率），并且桨叶转速在pH 7.5的0.2M磷酸盐缓冲液中的125rpm。

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