公开(公告)号：US20090048185A1

公开(公告)日：2009-02-19

申请号：US12084039

申请日：2006-10-27

申请人： Sachiko Miyake ,  Takashi Yamamura ,  Hirokazu Annoura

发明人： Sachiko Miyake ,  Takashi Yamamura ,  Hirokazu Annoura

IPC分类号： A61K31/7032 ,  C07H15/02 ,  A61P1/02 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P5/50 ,  A61P7/00 ,  A61P7/06 ,  A61P11/02 ,  A61P11/06 ,  A61P17/00 ,  A61P17/04 ,  A61P19/02 ,  A61P19/04 ,  A61P19/06 ,  A61P19/08 ,  A61P21/04 ,  A61P25/00 ,  A61P29/00 ,  A61P37/02

CPC分类号： A61K31/7032

摘要： A therapeutic drug for diseases, in which NKT cells or stimulus of NKT cells is involved in deterioration of disease conditions, containing, as an active ingredient, a glycolipid derivative having the formula (I): wherein R1 indicates an aldopyranose residue, R2 indicates a hydrogen atom or a hydroxy group, A indicates —CH2—, —CH(OH)—CH2— or —CH═CHCH2—, x indicates an integer of 13 to 16 and y indicates an integer of 0 to 25 or its pharmacologically acceptable hydrate or solvate.

摘要翻译： 一种治疗药物，其中NKT细胞或NKT细胞的刺激参与疾病病症的恶化，其含有具有式（I）的糖脂衍生物作为活性成分：其中R1表示吡喃葡萄糖残基，R2表示 氢原子或羟基，A表示-CH 2 - ， - CH（OH）-CH 2 - 或-CH-CHCH 2 - ，x表示13〜16的整数，y表示0〜25的整数或其药理学上可接受的水合物 或溶剂化物。

公开(公告)号：US07732583B2

公开(公告)日：2010-06-08

申请号：US10545421

申请日：2004-02-13

申请人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

发明人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

IPC分类号： C07G3/00 ,  C07H17/00 ,  C07H17/02 ,  A61K31/70 ,  A01N43/04

CPC分类号： C07D317/28 ,  C07C247/04 ,  C07H15/04 ,  C07H15/26

摘要： Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds.Glycolipids having the formula (I): where R3 indicates a substituted or unsubstituted C1 to C7 linear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and R8 indicates a substituted or unsubstituted C1 to C35 alkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

摘要翻译： 新型糖脂衍生物，其中鞘氨醇碱基部分的取代基为短碳链烷基，取代或未取代的环烷基，取代或未取代的芳基或取代或未取代的芳烷基，以及用于实际大量生产其的中间体的有效合成方法 可用于合成这些化合物。 具有式（I）的糖脂：其中R3表示取代或未取代的C1至C7直链烷基，取代或未取代的环烷基，取代或未取代的芳基或取代或未取代的芳烷基，R8表示取代或未取代的C1至C35 烷基，取代或未取代的芳基或取代或未取代的芳烷基是化学合成的。

公开(公告)号：US20060074235A1

公开(公告)日：2006-04-06

申请号：US10545421

申请日：2004-02-13

申请人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

发明人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

IPC分类号： C08B37/00

CPC分类号： C07D317/28 ,  C07C247/04 ,  C07H15/04 ,  C07H15/26

摘要： Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds. Glycolipids having the formula (I): where R3 indicates a substituted or unsubstituted C1 to C7 linear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and R8 indicates a substituted or unsubstituted C1 to C35 alkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

摘要翻译： 新型糖脂衍生物，其中鞘氨醇碱基部分的取代基为短碳链烷基，取代或未取代的环烷基，取代或未取代的芳基或取代或未取代的芳烷基，以及用于实际大规模生产的中间体的有效合成方法 可用于合成这些化合物。 具有式（I）的糖脂：其中R 3表示取代或未取代的C 1至C 7直链烷基，取代或未取代的环烷基 基团，取代或未取代的芳基或取代或未取代的芳烷基，R 8表示取代或未取代的C 1至C 35烷基的C 1〜 取代或未取代的芳基或取代或未取代的芳烷基是化学合成的。

公开(公告)号：US08034908B2

公开(公告)日：2011-10-11

申请号：US12760793

申请日：2010-04-15

申请人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

发明人： Hirokazu Annoura ,  Kenji Murata ,  Takashi Yamamura

IPC分类号： C07J9/00 ,  C07H17/02 ,  A01N43/04 ,  A61K31/70

CPC分类号： C07D317/28 ,  C07C247/04 ,  C07H15/04 ,  C07H15/26

摘要： Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds.Glycolipids having the formula (I): where R3 indicates a substituted or unsubstituted C1 to C7 linear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and R8 indicates a substituted or unsubstituted C1 to C35 alkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

摘要翻译： 新型糖脂衍生物，其中鞘氨醇碱基部分的取代基为短碳链烷基，取代或未取代的环烷基，取代或未取代的芳基或取代或未取代的芳烷基，以及用于实际大量生产其的中间体的有效合成方法 可用于合成这些化合物。 具有式（I）的糖脂：其中R3表示取代或未取代的C1至C7直链烷基，取代或未取代的环烷基，取代或未取代的芳基或取代或未取代的芳烷基，R8表示取代或未取代的C1至C35 烷基，取代或未取代的芳基或取代或未取代的芳烷基是化学合成的。

公开(公告)号：US20060178401A1

公开(公告)日：2006-08-10

申请号：US11337664

申请日：2006-01-24

申请人： Naohiro Takemoto ,  Hirokazu Annoura ,  Norihito Murayama

发明人： Naohiro Takemoto ,  Hirokazu Annoura ,  Norihito Murayama

IPC分类号： A61K31/454 ,  A61K31/445 ,  C07D211/56 ,  C07D401/02

CPC分类号： C07D417/04 ,  C07D211/58

摘要： The present invention relates to an amiophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q′, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C═O, NHC(═O), and C(═O)NH, and Q′ is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

摘要翻译： 本发明涉及式（I）的氨基苯氧基乙酰胺衍生物：其中R 1至R 4彼此独立地为氢原子或任选取代的烷基 组; E 1是-NR 4 - ; 并且E 2是氧原子或-NR 10 - ; Q是-XY-Q'基团，其中X和Y是连接键或X是亚烷基或亚烯基，Y选自CO，NHC（-O）和C（-O）NH的基团，和 Q'是氢原子或可被取代的苯基或吡啶基; 及其药学上可接受的盐。 本发明还涉及包含式（I）化合物和使用所述化合物治疗脑功能障碍和脑部有机疾病的方法的组合物。

公开(公告)号：US06998401B2

公开(公告)日：2006-02-14

申请号：US10394221

申请日：2003-03-24

申请人： Hirokazu Annoura ,  Naohiro Takemoto ,  Hiroshi Uramoto

发明人： Hirokazu Annoura ,  Naohiro Takemoto ,  Hiroshi Uramoto

IPC分类号： A61K31/445 ,  A61K31/535 ,  C07D211/80 ,  C07D401/00 ,  C07D217/02

CPC分类号： C07D401/06 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/58 ,  C07D401/12

摘要： There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1 and E2 are oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is pheny group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins.

摘要翻译： 提供下式（I）的氨基苯氧基乙酸衍生物：化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US06706734B2

公开(公告)日：2004-03-16

申请号：US10196362

申请日：2002-07-17

申请人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

发明人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

IPC分类号： A61K314465

CPC分类号： C07D211/44 ,  C07D211/12 ,  C07D211/14 ,  C07D211/18 ,  C07D211/52 ,  C07D211/70

摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.

摘要翻译： 一种药物组合物，特别是用于缓解或治疗由缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物，以及包含具有下式的芳基哌啶醇或芳基哌啶衍生物的Ca 2+过量抑制剂 I）：其中R为H，任选取代的苯基，任选取代的苯氧基或任选取代的苯甲酰基，A为任选被低级烷基取代的连接键，亚环烷基或亚烯基，B为任选取代的亚烷基 与OH或烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时， X不为H，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。

公开(公告)号：US07067533B2

公开(公告)日：2006-06-27

申请号：US10009566

申请日：2001-04-13

申请人： Naohiro Takemoto ,  Hirokazu Annoura ,  Norihito Murayama

发明人： Naohiro Takemoto ,  Hirokazu Annoura ,  Norihito Murayama

IPC分类号： A61K31/4468 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/58 ,  C07D215/00 ,  C07D217/00

CPC分类号： C07D417/04 ,  C07D211/58

摘要： The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q′, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C═O, NHC(═), and C(═O)NH, and Q′ is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

摘要翻译： 本发明涉及式（I）的氨基苯氧基乙酰胺衍生物：其中R 1至R 4彼此独立地为氢原子或任选取代的烷基 组; E 1是-NR 4 - ; 并且E 2是氧原子或-NR 10 - ; Q是-XY-Q'基团，其中X和Y是连接键或X是亚烷基或亚烯基，Y选自CO，NHC（ - ）和C（-O）NH，Q '是氢原子或可被取代的苯基或吡啶基; 及其药学上可接受的盐。 本发明还涉及包含式（I）化合物和使用所述化合物治疗脑功能障碍和脑部有机疾病的方法的组合物。

公开(公告)号：US06838470B2

公开(公告)日：2005-01-04

申请号：US10331508

申请日：2002-12-31

申请人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

发明人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

IPC分类号： A61P25/04 ,  A61K31/451 ,  A61K31/495 ,  A61P3/10 ,  A61P9/10 ,  A61P25/28 ,  C07C217/84 ,  C07C271/28 ,  C07D211/18 ,  C07D211/22 ,  C07D211/52 ,  C07D295/08 ,  C07D295/092 ,  C07D295/13 ,  C07D295/135

CPC分类号： C07D295/088 ,  C07C217/84 ,  C07C271/28 ,  C07D211/22 ,  C07D211/52 ,  C07D295/13 ,  Y02P20/55

摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

摘要翻译： 具有式（I）的化合物或其盐，水合物，水合物盐或溶剂化物：其中R 1至R 4独立地表示H，卤素，OH，烷氧基，任选取代的烷基，芳基或芳烷基，R 代表H，任选取代的烷基，芳基或芳烷基，E 1表示O，S或-NR 6，其中R 6表示H，任选取代的烷基，芳基或芳烷基 ，E 2表示O，S或-NR 7，其中R 7表示H，任选取代的烷基，芳基或芳烷基，A表示CH，C（OH）或N，X表示 H，卤素，烷氧基或任选取代的烷基，Q表示任选取代的苯基，苯氧基，苯甲基或环烷氧基，其中当E 1表示O或S时，E 2不表示O或 S具有抑制细胞毒性Ca 2+过载和脂质过氧化的作用，并且对于由于缺血性疾病等引起的症状缓解和治疗药物制剂有效。

公开(公告)号：US06455549B1

公开(公告)日：2002-09-24

申请号：US09043563

申请日：1998-03-20

申请人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

发明人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

IPC分类号： A61K31445

CPC分类号： C07D211/44 ,  C07D211/12 ,  C07D211/14 ,  C07D211/18 ,  C07D211/52 ,  C07D211/70

摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.

摘要翻译： 一种药物组合物，特别是用于缓解或治疗由于缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物和含有具有式（I）的芳基哌啶醇或芳基哌啶衍生物的Ca2 +过量抑制剂：其中 R是H，任意取代的苯基，任意取代的苯氧基或任选取代的苯甲酰基，A是任选被低级烷基取代的连接键，亚环烷基或亚烯基，B是任选被OH取代的亚烷基或 烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时，X不为H ，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。