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1. 发明授权

US08067396B2 Amino alcohol compounds or phosphonic acid derivatives thereof 有权
标题翻译：氨基醇化合物或其膦酸衍生物
公开(公告)号：US08067396B2
公开(公告)日：2011-11-29
申请号：US12460884
申请日：2009-07-24
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/675 , C07F9/28
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A compound having a formula II(a): wherein R1 and R2 are hydrogen lower alkyl, lower aliphatic acyl, or lower alkoxycarbonyl; R4 is C1-C4 alkyl; n is 2 or 3; X is a formula ═N-D, wherein D is hydrogen, C1-C6 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2—, —CH(OH)—CH2— or phenylene; Z is C1-C6 alkylene; R5 is C3-C10 cycloalkyl or C6-C10 aryl; R6 and R7 are hydrogen, lower alkyl, halogeno lower alkyl, lower alkoxy or lower alkylthio; and R10 and R11 are hydrogen or lower alkyl.
摘要翻译：具有式II（a）的化合物：其中R 1和R 2是氢低级烷基，低级脂族酰基或低级烷氧基羰基; R4是C1-C4烷基; n为2或3; X是式= N-D，其中D是氢，C 1 -C 6烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2 - ， - CH（OH）-CH 2 - 或亚苯基; Z是C1-C6亚烷基; R5是C3-C10环烷基或C6-C10芳基; R6和R7是氢，低级烷基，卤代低级烷基，低级烷氧基或低级烷硫基; R 10和R 11为氢或低级烷基。

2. 发明授权

US07199150B2 Amino alcohol compounds 有权
标题翻译：氨基醇化合物
公开(公告)号：US07199150B2
公开(公告)日：2007-04-03
申请号：US10889657
申请日：2004-07-12
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein R1 and R2 each represent hydrogen, or a protecting group of the amino group; R3 represents hydrogen, or a protecting group of the hydroxyl group; R4 represents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C1–C10 alkylene; R5 represents an aryl group; and R6 and R7 each represents hydrogen; provided that when R5 represents hydrogen, then Z represents a group other than a single bond or a straight chain C1–C10 alkylene group.
摘要翻译：具有优异的免疫抑制活性的氨基醇化合物和膦酸化合物，其药学上可接受的盐和药理学上可接受的酯，以及包含这些化合物的药物组合物，具有下式的化合物：

3. 发明申请

US20070105933A1 Amino alcohol compounds 审中-公开
标题翻译：氨基醇化合物
公开(公告)号：US20070105933A1
公开(公告)日：2007-05-10
申请号：US11636776
申请日：2006-12-11
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A method for the preventing a disease selected from the group consisting of rheumatoid arthritis and psoriasis in a mammal, such as a human, in need thereof, which includes administering to the mammal a pharmaceutically effective amount of a compound of formula (Ia) wherein R1 and R2 are each hydrogen; R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is=N-D, wherein D is hydrogen, C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is an unsubstituted C3-C10 cycloalkyl, an unsubstituted C6-C10 aryl, or a C3-C10 cycloalkyl or C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.
摘要翻译：一种用于预防在有需要的哺乳动物（例如人）中选自类风湿性关节炎和牛皮癣的疾病的方法，其包括向所述哺乳动物施用药学有效量的式（Ia）化合物，其中R lt; 1＆gt;和＆lt; 2＆gt; 2＆lt; 2＆gt;各为氢; R 3是氢; R 4是C 1 -C 2烷基; R 4是C 1 -C 2烷基; n为2; X是= N-D，其中D是氢，C 1 -C 4烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2或亚苯基; Z是乙烯或三亚甲基; R 5是未取代的C 3 -C 10环烷基，未取代的C 6 -C 10环烷基芳基或C 3 -C 10环烷基或C 6 -C 10 - 芳基取代的（C 1 -C 6）芳基，具有1至3个选自卤素，低级烷基，卤代低级烷基和低级烷氧基的取代基; R 6和R 7均为氢。

4. 发明授权

US07910617B2 Method for suppressing the number of peripheral blood lymphocytes using an amino alcohol compound 有权
标题翻译：使用氨基醇化合物抑制外周血淋巴细胞数的方法
公开(公告)号：US07910617B2
公开(公告)日：2011-03-22
申请号：US10588818
申请日：2005-02-23
申请人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
发明人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
IPC分类号： A61K31/40
CPC分类号： A61K31/40
摘要： A method for suppressing the number of peripheral blood lymphocytes involving administering to a human in need thereof a pharmaceutically effective amount of a compound which is (2R) -2-amino-2-methyl-4-{1-methyl-5-[4-(4-methylphenyl)butanoyl]pyrrol-2-yl}butan-1-ol or a pharmacologically acceptable salt thereof, such as the hydrochloride salt.
摘要翻译：一种抑制外周血淋巴细胞数量的方法，包括向有需要的人施用药学有效量的化合物，其是（2R）-2-氨基-2-甲基-4- {1-甲基-5- [4 - （4-甲基苯基）丁酰基]吡咯-2-基}丁-1-醇或其药理学上可接受的盐，例如盐酸盐。

5. 发明申请

US20070191468A1 Amino alcohol compound 有权
标题翻译：氨基醇化合物
公开(公告)号：US20070191468A1
公开(公告)日：2007-08-16
申请号：US10588818
申请日：2005-02-23
申请人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
发明人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
IPC分类号： A61K31/401 , A61P1/04
CPC分类号： A61K31/40
摘要： A pharmaceutical composition is provided that has a low toxicity, demonstrates superior physicochemical properties and pharmacokinetics, and has superior peripheral blood lymphocyte count lowering activity. The pharmaceutical composition contains a compound having general formula (I): [Chemical Formula 1] (wherein R1 represents a methyl group or an ethyl group, R2 represents a methyl group or an ethyl group, and R3 represents a phenyl group substituted with 1 to 3 substituents selected from the group consisting of a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, a halogeno lower alkyl group, a lower aliphatic acyl group and a cyano group), a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof.
摘要翻译：提供毒性低的药物组合物，具有优异的物理化学性质和药代动力学，并且具有优异的外周血淋巴细胞计数降低活性。药物组合物含有具有通式（I）的化合物：[化学式1]（其中R 1表示甲基或乙基，R 2表示甲基基团或乙基，R 3表示被1〜3个选自卤素原子，低级烷基，环烷基，低级烷氧基，低级烷氧基，卤代低级烷基，低级脂肪酰基和氰基），其药学上可接受的盐或其药理学上可接受的酯。

6. 发明授权

US07638551B2 Amino alcohol compounds or phosphonic acid derivatives thereof 有权
标题翻译：氨基醇化合物或其膦酸衍生物
公开(公告)号：US07638551B2
公开(公告)日：2009-12-29
申请号：US11651205
申请日：2007-01-09
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A method for the prevention or treatment of an immunology-related disease, which is not rheumatoid arthritis or psoriasis, in a mammal in need thereof which involves administering to the mammal a pharmaceutically effective amount of a compound, a pharmacologically acceptable salt of the compound or a pharmacologically acceptable ester of the compound, wherein the compound is a compound having a formula (Ia): wherein R1 and R2 are each a hydrogen, R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ═N—D, wherein D is hydrogen C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is an unsubstituted C3-C10 cycloalkyl, an unsubstituted C6-C10 aryl, or a C3-C10 cycloalkyl or a C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.
摘要翻译：一种在有需要的哺乳动物中预防或治疗免疫学相关疾病（其不是类风湿性关节炎或牛皮癣）的方法，其涉及向所述哺乳动物施用药学有效量的化合物，所述化合物的药理学上可接受的盐或化合物的药理学上可接受的酯，其中所述化合物是具有式（Ia）的化合物：其中R 1和R 2各自为氢，R 3为氢; R4是C1-C2烷基; n为2; X是-N-D，其中D是氢C1-C4烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2或亚苯基; Z是乙烯或三亚甲基; R5是未取代的C 3 -C 10环烷基，未取代的C 6 -C 10芳基或C 3 -C 10环烷基或被1至3个选自卤素，低级烷基，卤代低级烷基和低级烷基的取代基取代的C 6 -C 10芳基烷氧基 R6和R7各自为氢。

7. 发明申请

US20050043386A1 Amino alcohol derivatives or phosphonic acid derivatives and pharmaceutical compositions containing these 有权
标题翻译：氨基醇衍生物或膦酸衍生物和含有这些的药物组合物
公开(公告)号：US20050043386A1
公开(公告)日：2005-02-24
申请号：US10889657
申请日：2004-07-12
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： C07D307/52 , A61K20060101 , A61K31/34 , A61K31/40 , A61K31/42 , A61K31/436 , A61K31/519 , A61K31/661 , A61K31/662 , A61K38/00 , A61K39/395 , A61K45/00 , A61P20060101 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P43/00 , C07D20060101 , C07D207/32 , C07D207/335 , C07D333/20 , C07F9/572 , C07F9/653 , C07F9/655 , C07F9/6553 , C07D207/46 , C07D307/02
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein R1 and R2 each represent hydrogen, or a protecting group of the amino group; R3 represents hydrogen, or a protecting group of the hydroxyl group; R4 represents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C1-C10 alkylene; R5 represents an aryl group; and R6 and R7 each represents hydrogen; provided that when R5 represents hydrogen, then Z represents a group other than a single bond or a straight chain C1-C10 alkylene group.
摘要翻译：具有优异的免疫抑制活性的氨基醇化合物和膦酸化合物，其药理学上可接受的盐和药理学上可接受的酯，以及包含这些化合物的药物组合物，具有下式的化合物：其中R 1和R 2各自代表氢，或氨基的保护基; R 3表示氢或羟基的保护基; R 4表示低级烷基; n为1至6; X表示氧或氮，未取代或被低级烷基取代; Y表示乙烯; Z表示C1-C10亚烷基; R 5表示芳基; R 6和R 7各自表示氢; 条件是当R 5表示氢时，则Z表示除单键或直链C1-C10亚烷基以外的基团。

8. 发明授权

US08101650B2 Method for treating a immunology-related disease 有权
标题翻译：治疗免疫学相关疾病的方法
公开(公告)号：US08101650B2
公开(公告)日：2012-01-24
申请号：US12583001
申请日：2009-08-12
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A method for treating an immunology-related disease. The method involves administering to a mammal in need thereof a pharmaceutically effective amount of an amino acid compound, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. The compound has the following formula: wherein R1 and R2 are each hydrogen; R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ═N-D, wherein D is hydrogen, C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is unsubstituted C3-C10 cycloalkyl, unsubstituted C3-C10 aryl, or C3-C10 cycloalkyl or C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.
摘要翻译：一种治疗免疫学相关疾病的方法。该方法涉及向有需要的哺乳动物施用药学有效量的氨基酸化合物，其药理学上可接受的盐或其药理学上可接受的酯。该化合物具有下式：其中R1和R2各自为氢; R3是氢; R4是C1-C2烷基; n为2; X是= N-D，其中D是氢，C 1 -C 4烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2或亚苯基; Z是乙烯或三亚甲基; R5是未取代的C3-C10环烷基，未取代的C3-C10芳基或被1至3个选自卤素，低级烷基，卤代低级烷基和低级烷氧基的取代基取代的C 3 -C 10环烷基或C 6 -C 10芳基; R6和R7各自为氢。

9. 发明申请

US20090326038A1 Method for treating a immunology-related disease 有权
标题翻译：治疗免疫学相关疾病的方法
公开(公告)号：US20090326038A1
公开(公告)日：2009-12-31
申请号：US12583001
申请日：2009-08-12
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40 , A61P37/00
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A method for treating an immunology-related disease. The method involves administering to a mammal in need thereof a pharmaceutically effective amount of an amino acid compound, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. The compound has the following formula: , wherein R1 and R2 are each hydrogen; R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ═N-D, wherein D is hydrogen, C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is unsubstituted C3-C10 cycloalkyl, unsubstituted C3-C10 aryl, or C3-C10 cycloalkyl or C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.
摘要翻译：一种治疗免疫学相关疾病的方法。该方法涉及向有需要的哺乳动物施用药学有效量的氨基酸化合物，其药理学上可接受的盐或其药理学上可接受的酯。该化合物具有下式：其中R 1和R 2各自为氢; R3是氢; R4是C1-C2烷基; n为2; X是-N-D，其中D是氢，C 1 -C 4烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2或亚苯基; Z是乙烯或三亚甲基; R5是未取代的C3-C10环烷基，未取代的C3-C10芳基或被1至3个选自卤素，低级烷基，卤代低级烷基和低级烷氧基的取代基取代的C 3 -C 10环烷基或C 6 -C 10芳基; R6和R7各自为氢。

10. 发明申请

US20070142335A1 Amino alcohol compounds or phosphonic acid derivatives thereof 有权
标题翻译：氨基醇化合物或其膦酸衍生物
公开(公告)号：US20070142335A1
公开(公告)日：2007-06-21
申请号：US11651205
申请日：2007-01-09
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/675 , A61K31/40 , A61K31/401 , C07F9/572
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A method for the prevention or treatment of an immunology-related disease, which is not rheumatoid arthritis or psoriasis, in a mammal in need thereof which involves administering to the mammal a pharmaceutically effective amount of a compound, a pharmacologically acceptable salt of the compound or a pharmacologically acceptable ester of the compound, wherein the compound is a compound having a formula (Ia): wherein R1 and R2 are each a hydrogen, R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ═N-D, wherein D is hydrogen C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is an unsubstituted C3-C10 cycloalkyl, an unsubstituted C6-C10 aryl, or a C3-C10 cycloalkyl or a C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.
摘要翻译：一种在有需要的哺乳动物中预防或治疗免疫学相关疾病（其不是类风湿性关节炎或牛皮癣）的方法，其涉及向所述哺乳动物施用药学有效量的化合物，所述化合物的药理学上可接受的盐或化合物的药理学上可接受的酯，其中所述化合物是具有式（Ia）的化合物：其中R 1和R 2各自为氢，R 1， 3是氢; R 4是C 1 -C 2烷基; R 4是C 1 -C 2烷基; n为2; X是-N-D，其中D是氢C 1 -C 4烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2或亚苯基; Z是乙烯或三亚甲基; R 5是未取代的C 3 -C 10环烷基，未取代的C 6 -C 10环烷基芳基或C 3 -C 10环烷基或C 6 -C 10 - 芳基被1至3个选自卤素，低级烷基，卤代低级烷基和低级烷氧基的取代基取代; R 6和R 7均为氢。

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