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1. 发明授权

US06291432B1 Tripeptide compounds and anti-AIDS medicine 失效
标题翻译：三肽化合物和抗艾滋病药物
公开(公告)号：US06291432B1
公开(公告)日：2001-09-18
申请号：US09155773
申请日：1999-02-16
申请人： Haruo Takaku , Satoshi Nojima , Tsutomu Mimoto , Keisuke Terashima , Yoshiaki Kiso
发明人： Haruo Takaku , Satoshi Nojima , Tsutomu Mimoto , Keisuke Terashima , Yoshiaki Kiso
IPC分类号： A61K3806
CPC分类号： C07D263/04 , C07D277/06 , C07D417/12 , C07K5/0202
摘要： A novel tripeptide compound represented by the following general formula (I) exhibiting superior HIV protease inhibition activity, and an anti-AIDS medicine comprising this compound as an effective component and a pharmaceutically acceptable salt thereof. (R)-N-(2-methylbenzyl)-3-{(2S,3S)-3-[N-(2-chromonecarbonyl)-L-asparaginyl]amino-2-hydroxy-4-phenylbutanoyl}-5,5-dimethyl-1,3-thiazolidine-4-carboxamide can be given as a typical example of this compound.
摘要翻译：由下述通式（I）表示的具有优异的HIV蛋白酶抑制活性的新型三肽化合物和包含该化合物作为有效成分的抗艾滋病药物，（R）-N-（2-甲基苄基）-3 - {（2S，3S）-3- [N-（2-色烯羰基）-L-天冬酰胺基]氨基-2-羟基-4-苯基丁酰基} -5,5-二甲基-1,3-噻唑烷-4 甲酰胺可以作为该化合物的典型实例给出。

2. 发明授权

US06222043B1 Methods of preparing novel dipeptide compounds or pharmaceutically acceptable salts thereof 有权
标题翻译：制备新型二肽化合物或其药学上可接受的盐的方法
公开(公告)号：US06222043B1
公开(公告)日：2001-04-24
申请号：US09228009
申请日：1999-01-08
申请人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
发明人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
IPC分类号： C07D27706
CPC分类号： C07D263/06 , C07D207/16 , C07D277/06
摘要： The present invention provides synthetic methodology to produce novel dipeptide compounds and pharmaceutically acceptable salts thereof which exhibit excellent HIV protease inhibitory activity and excellent bioavailability from digestive tracts. Methods of using the dipeptide compounds and pharmaceutically acceptable salts thereof also are provided. A non-limiting example of a dipeptide compound of the invention has the general formula (IA): where R1 represents a 5-membered or 6-membered monocyclic hydrocarbon group or heterocyclic group wherein 3 or fewer substituents other than hydrogen are present on the cyclic group; R21 and R22 each represents a hydrogen atom or a linear or branched aliphatic hydrocarbon group having 1-6 carbon atoms; and R3 represents a linear or branched aliphatic hydrocarbon group having 1-6 carbon atoms or a monovalent group comprising an aromatic monocyclic hydrocarbon group having 12 or fewer carbon atoms in total, wherein a halogen atom can be substituted on the aromatic ring of the aromatic monocyclic hydrocarbon group.
摘要翻译：本发明提供合成方法以产生新的二肽化合物及其药学上可接受的盐，其表现出优异的HIV蛋白酶抑制活性和从消化道获得优异的生物利用度。还提供了使用二肽化合物及其药学上可接受的盐的方法。本发明的二肽化合物的非限制性实例具有通式（IA）：其中R 1表示5元或6元单环烃基或杂环基，其中3个或更少个除氢以外的取代基存在于环状组; R 21和R 22各自表示氢原子或具有1-6个碳原子的直链或支链脂族烃基; R3表示具有1-6个碳原子的直链或支链脂族烃基或包含总共具有12个或更少碳原子的芳族单环烃基的一价基团，其中卤素原子可以在芳族单环的芳环上被取代烃基。

3. 发明授权

US5962640A Methods for preparing novel dipeptide compounds or pharmacuetically acceptable salts thereof 有权
标题翻译：制备新型二肽化合物或其药学上可接受的盐的方法
公开(公告)号：US5962640A
公开(公告)日：1999-10-05
申请号：US137608
申请日：1998-08-21
申请人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
发明人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
IPC分类号： C07D207/16 , C07D263/06 , C07D277/06 , C07K1/06 , A61K38/05 , C07K5/06
CPC分类号： C07D277/06 , C07D207/16 , C07D263/06
摘要： The present invention provides a novel dipeptide compound or pharmaceutically acceptable salt thereof which exhibits an excellent HIV protease inhibitory activity and an excellent bioavailability from digestive tracts, and an anti-AIDS agent comprising said dipeptide compound as an effective ingredient. ##STR1## (wherein R.sub.1 represents 5-membered or 6-membered monocyclic hydrocarbon group or heterocyclic group wherein more than one carbon atom of said monocyclic hydrocarbon group is substituted with hetero atom. X represents methylene group (--CH.sub.2 --), chloromethylene group(--CH(Cl)--), oxygen atom sulfur atom or sulfonyl group (--SO.sub.2 --). R.sub.21 and R.sub.22 each represents hydrogen atom or aliphatic hydrocarbon group having 1-6 carbons. R.sub.3 represents aliphatic hydrocarbon group or monovalent group derived from aromatic monocyclic hydrocarbon having 1-6 carbons.)
摘要翻译：本发明提供了一种新的二肽化合物或其药学上可接受的盐，其表现出优异的HIV蛋白酶抑制活性和来自消化道的优异生物利用度，以及包含所述二肽化合物作为有效成分的抗AIDS剂。（其中R1表示5元或6元单环烃基或杂环基，其中所述单环烃基的多于一个碳原子被杂原子取代，X表示亚甲基（-CH 2 - ），氯亚甲基（-CH（ Cl） - ），氧原子硫原子或磺酰基（-SO 2 - ），R 21和R 22各自表示氢原子或具有1-6个碳的脂族烃基，R3表示脂族烃基或由具有1个 -6碳。

4. 发明授权

US06399568B1 Cyclic tetrapeptide derivatives and medicinal use thereof 失效
标题翻译：环状四肽衍生物及其医药用途
公开(公告)号：US06399568B1
公开(公告)日：2002-06-04
申请号：US09486783
申请日：2000-03-01
申请人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu , Tsutomu Mimoto
发明人： Norikazu Nishino , Minoru Yoshida , Sueharu Horinouchi , Yasuhiko Komatsu , Tsutomu Mimoto
IPC分类号： A61K3812
CPC分类号： C07K5/126 , A61K38/00
摘要： A cyclic tetrapeptide derivative represented by the general formula (I): wherein: R11, R12, R21 and R22 independently denote a monovalent group selected from hydrogen, a linear or branched alkyl group with 6 or less carbon atoms, benzyl group, 4-methoxybenzyl group, 3-indolylmethyl group, (N-methoxy-3-indolyl) methyl group, (N-formyl-3-indolyl)methyl group, etc.; R3 denotes a divalent group selected from a linear chained hydrocarbon group with 3 or 4 carbon atoms, or the linear branched hydrocarbon group having a branched chain added to the chain, or a divalent group substituted with a heteroatom; R4 denotes a divalent chained hydrocarbon group with 4 to 6 carbon atoms, or a divalent group derived from said hydrocarbon group by addition etc. of a branched chain on said chain; and a pharmaceutically acceptable salt thereof, or an analogous cyclic tetrapeptide derivative compound; as well as a histone deacetylase enzyme inhibitor, an MHC class-I molecule expression promoting agent and a pharmaceutical composition that comprise said cyclic tetrapeptide derivative as an effective ingredient.
摘要翻译：由通式（I）表示的环状四肽衍生物：其中：R11，R12，R21和R22独立地表示选自氢，碳原子数6以下的直链或支链烷基，苄基，4-甲氧基苄基（3-甲氧基-3-吲哚基）甲基，（N-甲酰基-3-吲哚基）甲基等。 R3表示选自具有3或4个碳原子的直链状烃基或者在该链上添加有支链的直链支链烃基或被杂原子取代的二价基团的二价基团; R4表示二价链状烃基或含有4〜6个碳原子的二价基团，或通过所述链上的支链的加成等衍生自所述烃基的二价基团; 和其药学上可接受的盐，或类似的环状四肽衍生物化合物; 以及组蛋白脱乙酰酶酶抑制剂，MHC class I分子表达促进剂和包含所述环状四肽衍生物作为有效成分的药物组合物。

5. 发明授权

US5932550A Dipeptide compound or pharmaceutically acceptable salt thereof and medical use thereof 失效
标题翻译：二肽化合物或其药学上可接受的盐及其医疗用途
公开(公告)号：US5932550A
公开(公告)日：1999-08-03
申请号：US669757
申请日：1996-06-26
申请人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
发明人： Ryohei Kato , Tsutomu Mimoto , Tominaga Fukazawa , Naoko Morohashi , Yoshiaki Kiso
IPC分类号： C07D207/16 , C07D263/06 , C07D277/06 , A61K38/05 , C07K1/06 , C07K5/06
CPC分类号： C07D277/06 , C07D207/16 , C07D263/06
摘要： The present invention provides a novel dipeptide compound or pharmaceutically acceptable salt thereof which exhibits an excellent HIV protease inhibitory activity and an excellent bioavailability from digestive tracts, and an anti-AIDS agent comprising said dipeptide compound as an effective ingredient.General formula (I): ##STR1## (wherein R.sub.1 represents 5-membered or 6-membered monocyclic hydrocarbon group or heterocyclic group wherein more than one carbon atom of said monocyclic hydrocarbon group is substituted with hetero atom. X represents methylene group (--CH.sub.2 --), chloromethylene group(--CH(Cl)--), oxygen atom sulfur atom or sulfonyl group (--SO.sub.2 --). R.sub.21 and R.sub.22 each represents hydrogen atom or aliphatic hydrocarbon group having 1-6 carbons. R.sub.3 represents aliphatic hydrocarbon group or monovalent group derived from aromatic monocyclic hydrocarbon having 1-6 carbons.)
摘要翻译：本发明提供了一种新的二肽化合物或其药学上可接受的盐，其表现出优异的HIV蛋白酶抑制活性和来自消化道的优异生物利用度，以及包含所述二肽化合物作为有效成分的抗AIDS剂。通式（I）：（其中R1表示5元或6元单环烃基或杂环基，其中所述单环烃基中多于一个碳原子被杂原子取代，X表示亚甲基（-CH 2 - ），氯亚甲基（-CH（Cl） - ），氧原子硫原子或磺酰基（-SO 2 - ），R 21和R 22各自表示氢原子或具有1-6个碳的脂肪族烃基，R3表示脂肪族烃基或一价基团具有1-6个碳原子的芳族单环烃。

6. 发明申请

US20090198056A1 Beta secretase inhibitor 失效
标题翻译： β分泌酶抑制剂
公开(公告)号：US20090198056A1
公开(公告)日：2009-08-06
申请号：US11991426
申请日：2006-08-31
申请人： Tsutomu Mimoto , Satoshi Nojima , Naoya Kinomura , Yoshiaki Kiso
发明人： Tsutomu Mimoto , Satoshi Nojima , Naoya Kinomura , Yoshiaki Kiso
IPC分类号： C07D403/12 , C07D405/12 , C07D233/88 , C07D235/30 , C07D257/06
CPC分类号： C07D233/88 , C07C279/22 , C07D235/30 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.
摘要翻译：本发明涉及式（1）的化合物：其中R1是式（2）的基团：其中X是氮原子或C（R5），Y是氮原子或C（R6），R5和R6 各自独立地为氢原子等）等，m为1〜6，L1为单键等，R2为氢原子，取代或未取代的烷基等，R3为氢原子等，L2为单键等，R4为氢原子，取代或未取代的芳基等，或其药学上可接受的盐，可用于预防或治疗阿尔茨海默病。

7. 发明授权

US06329502B1 &bgr;-amino-&agr;-hydroxycarboxylic acid derivatives and HIV protease inhibitors 失效
公开(公告)号：US06329502B1
公开(公告)日：2001-12-11
申请号：US08378057
申请日：1995-01-25
申请人： Tsutomu Mimoto , Naoko Hattori , Makoto Shintani , Yuuichi Nagano , Yoshiaki Kiso
发明人： Tsutomu Mimoto , Naoko Hattori , Makoto Shintani , Yuuichi Nagano , Yoshiaki Kiso
IPC分类号： C07K508
CPC分类号： C07K5/0202 , C07K7/02
摘要： &bgr;-Amino-&agr;-hydroxycarboxylic acid derivatives represented by the following formula and salts thereof which are useful as human immunodeficiency virus (HIV) protease inhibitors: The compounds are effective for treating a patient suffering from AIDS and AIDS related diseases.

8. 发明授权

US06313094B1 &bgr;-amino-&agr;-hydroxycarboxylic acid derivatives and HIV protease inhibitors 失效
标题翻译： β-氨基-α-羟基羧酸衍生物和HIV蛋白酶抑制剂
公开(公告)号：US06313094B1
公开(公告)日：2001-11-06
申请号：US08246843
申请日：1994-05-20
申请人： Tsutomu Mimoto , Naoko Hattori , Makoto Shintani , Yuuichi Nagano , Yoshiaki Kiso
发明人： Tsutomu Mimoto , Naoko Hattori , Makoto Shintani , Yuuichi Nagano , Yoshiaki Kiso
IPC分类号： C07K508
CPC分类号： C07K5/0202 , C07K7/02
摘要： &bgr;-Amino-&agr;-hydroxycarboxylic acid derivatives represented by the following formula and salts thereof which are useful as human immunodeficiency virus (HIV) protease inhibitors: The compounds are effective for treating a patient suffering from AIDS and AIDS related diseases.
摘要翻译：由下式表示的β-氨基-α-羟基羧酸衍生物及其盐，其可用作人类免疫缺陷病毒（HIV）蛋白酶抑制剂：该化合物对于治疗患有艾滋病和AIDS相关疾病的患者是有效的。

9. 发明授权

US5644028A Process for producing peptide derivatives and salts therefor 失效
标题翻译：生产肽衍生物及其盐的方法
公开(公告)号：US5644028A
公开(公告)日：1997-07-01
申请号：US364707
申请日：1994-12-28
申请人： Tsutomu Mimoto , Sumitsugu Kisanuki , Osamu Takahashi , Yoshiaki Kiso
发明人： Tsutomu Mimoto , Sumitsugu Kisanuki , Osamu Takahashi , Yoshiaki Kiso
IPC分类号： C07C319/14 , C07C323/59 , C07D277/06 , C07D417/12 , C07K1/02 , C07K1/08 , C07K1/10 , C07K5/083
CPC分类号： C07D417/12 , C07C319/14 , C07D277/06
摘要： A process for producing peptide derivatives of formula (1) or salts thereof: ##STR1## which comprises condensation of peptide derivative of formula (2): ##STR2## with carboxylic acid of formula (3): ##STR3## or condensation of a peptide derivative of formula (4): ##STR4## with a protected amino acid of formula (5'): ##STR5## wherein R.sup.1 and R.sup.2 are a lower alkyl group or hydrogen atom, R.sup.3 is a lower alkyl group, X is a methylthiomethyl, methanesulfonylmethyl, carbamoylmethyl, or a lower alkyl group, Ar is an aryl or heteroaryl group, and A.sup.4 is Ar--O--CH.sub.2 --CO. The peptide derivatives and salts thereof are useful as the human immunodeficiency virus (HIV) protease inhibitors.
摘要翻译：（1）的肽衍生物或其盐的制备方法：包括式（2）的肽衍生物与式（3）的羧酸缩合的式（1）：IMA图（3）或式（4）的肽衍生物与式（5'）的保护的氨基酸的缩合：其中R 1和R 2是低级烷基或氢原子，R3是低级烷基，X是甲硫基甲基，甲磺酰基甲基，氨基甲酰基甲基或低级烷基，Ar是芳基或杂芳基，A4是Ar-O-CH2-CO。肽衍生物及其盐可用作人类免疫缺陷病毒（HIV）蛋白酶抑制剂。

10. 发明授权

US07816387B2 β secretase inhibitor 失效
标题翻译：＆bgr 分泌酶抑制剂
公开(公告)号：US07816387B2
公开(公告)日：2010-10-19
申请号：US11991426
申请日：2006-08-31
申请人： Tsutomu Mimoto , Satoshi Nojima , Naoya Kinomura , Yoshiaki Kiso
发明人： Tsutomu Mimoto , Satoshi Nojima , Naoya Kinomura , Yoshiaki Kiso
IPC分类号： A61K31/4168 , A61K31/4196 , A61K31/41 , C07D233/88 , C07D249/14 , C07D257/06
CPC分类号： C07D233/88 , C07C279/22 , C07D235/30 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.
摘要翻译：本发明涉及式（1）的化合物：其中R1是式（2）的基团：其中X是氮原子或C（R5），Y是氮原子或C（R6），R5和R6 各自独立地为氢原子等）等，m为1〜6，L1为单键等，R2为氢原子，取代或未取代的烷基等，R3为氢原子等，L2为单键等，R4为氢原子，取代或未取代的芳基等，或其药学上可接受的盐，可用于预防或治疗阿尔茨海默病。

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