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1. 发明授权

US5300634A Process for producing maltooligosaccharide derivative 失效
标题翻译：生产麦芽低聚糖衍生物的方法
公开(公告)号：US5300634A
公开(公告)日：1994-04-05
申请号：US878266
申请日：1992-05-04
申请人： Atsunori Sano , Naoki Teno
发明人： Atsunori Sano , Naoki Teno
IPC分类号： C07H3/06 , C12Q1/40 , C07H15/00
CPC分类号： C12Q1/40 , C07H3/06 , C12Q2334/10
摘要： A maltooligosaccharide derivative very useful, for example, as a precursor of a modified oligosaccharide derivative having one or more modifying groups at the 6-position or the 4- and 6-positions of the non-reducing end glucose residue which can be effectively used as a substrate for determining .alpha.-amylase activity or an intermediate thereof, can be produced by reacting a compound of the formula: ##STR1## with a compound of the formula: ##STR2## to convert at least the hydroxyl groups at the 4- and 6-positions of non-reducing end glucose residue of the compound of the formula (1) into a cyclic boric acid ester, acylating the reaction product, and then treating the acylated product.
摘要翻译：非常有用的麦芽低聚糖衍生物，例如作为在非还原性末端葡萄糖残基的6位或4位和6位上具有一个或多个修饰基团的修饰的寡糖衍生物的前体，其可以有效地用作用于确定（α） - 淀粉酶活性的底物或其中间体可以通过使下式化合物：（* CHEMICAL STRUCTURE *）（1）与下式化合物反应来制备：（* CHEMICAL STRUCTURE *）（2 ）将至少将式（1）化合物的非还原性末端葡萄糖残基的4-位和6-位的羟基转化成环状硼酸酯，酰化反应产物，然后处理酰化产物。

2. 发明申请

US20050054851A1 Pyrrolo pyrimidines as agents for the inhibition of cystein proteases 失效
标题翻译：吡咯并嘧啶作为抑制半胱氨酸蛋白酶的药剂
公开(公告)号：US20050054851A1
公开(公告)日：2005-03-10
申请号：US10487760
申请日：2002-08-29
申请人： Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D473/00 , C07D487/04 , C07D519/00 , C07D473/10
CPC分类号： C07D487/04 , C07D473/00
摘要： The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或酯，其中符号具有如上定义的含义，其是组织蛋白酶K的抑制剂，并且可用于药物治疗用于治疗组织蛋白酶K的疾病和医学病症。各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症和肿瘤。

3. 发明授权

US07820818B2 Heteroaryl nitrile derivatives 失效
标题翻译：杂芳基腈衍生物
公开(公告)号：US07820818B2
公开(公告)日：2010-10-26
申请号：US12399761
申请日：2009-03-06
申请人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： C07D239/47 , C07D239/48 , A61K31/505 , A61K31/506 , A61P19/02
CPC分类号： C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34
摘要： The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或酯，其中符号具有如上定义的含义，其是组织蛋白酶K的抑制剂，并且可用于药物治疗用于组织蛋白酶K的疾病和医学病症。各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症和肿瘤。

4. 发明授权

US07544688B2 Hetereoaryl nitrile derivatives 失效
标题翻译：异丁酰腈衍生物
公开(公告)号：US07544688B2
公开(公告)日：2009-06-09
申请号：US10525658
申请日：2003-08-29
申请人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： C07D239/47 , C07D239/48 , A61K31/505 , A61K31/506 , A61P19/02
CPC分类号： C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34
摘要： The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或酯，其中符号具有如上所定义的含义，其是组织蛋白酶K的抑制剂，并且可用于药物治疗用于组织蛋白酶K的疾病和医学病症。各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症和肿瘤。

5. 发明授权

US06353017B1 Dipeptide nitriles 失效
标题翻译：二肽腈
公开(公告)号：US06353017B1
公开(公告)日：2002-03-05
申请号：US09643639
申请日：2000-08-22
申请人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry van Duzer
发明人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry van Duzer
IPC分类号： A61K3140
CPC分类号： C07C255/29 , C07C255/44 , C07C271/22 , C07C317/44 , C07C323/52 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D207/327 , C07D209/18 , C07D209/42 , C07D211/06 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/64 , C07D241/44 , C07D249/06 , C07D261/18 , C07D275/02 , C07D295/088 , C07D295/15 , C07D295/155 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/85 , C07D317/68 , C07D333/24 , C07D333/38 , C07D333/40 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06043 , C07K5/06078
摘要： N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
摘要翻译：定义的N-末端取代的二肽腈可用作半胱氨酸组织蛋白酶的抑制剂，例如，组织蛋白酶B，K，L和S，可用于治疗半胱氨酸组织蛋白酶依赖性疾病和病症，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症，肿瘤（特别是肿瘤侵袭和肿瘤转移），冠状动脉疾病，动脉粥样硬化（包括动脉粥样硬化斑块破裂和不稳定）。特定的二肽腈是式I化合物或生理上可接受的和可切割的酯或其盐，其中符号如上所定义。特别地，已经发现通过适当选择基团R，R 2，R 3，R 4，R 5， X1，Y和L，化合物作为各种半胱氨酸组织蛋白酶类型的抑制剂的相对选择性，例如组织蛋白酶B，K，L和S可以被改变，例如，以获得选择性抑制特定组织蛋白酶类型或组织蛋白酶类型组合的抑制剂。

6. 发明申请

US20090227596A1 HETEROARYL NITRILE DERIVATIVES 失效
标题翻译：异丙肾上腺素衍生物
公开(公告)号：US20090227596A1
公开(公告)日：2009-09-10
申请号：US12399761
申请日：2009-03-06
申请人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Eva Altmann , Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： A61K31/496 , C07D239/02 , A61K31/505 , A61P29/00 , A61P19/02 , A61P37/00 , A61P35/00 , A61P9/00
CPC分类号： C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34
摘要： The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或酯，其中符号具有如上定义的含义，其是组织蛋白酶K的抑制剂，并且可用于药物治疗用于组织蛋白酶K的疾病和医学病症。各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症和肿瘤。

7. 发明申请

US20090054467A1 Pyrrolo Pyrimidines as Agents for the Inhibition of Cystein Proteases 审中-公开
标题翻译：吡咯并嘧啶类作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US20090054467A1
公开(公告)日：2009-02-26
申请号：US12237896
申请日：2008-09-25
申请人： Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Claudia Betschart , Kenji Hayakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： A61K31/52 , C07D473/00
CPC分类号： C07D487/04 , C07D473/00
摘要： The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或酯，其中符号具有如上定义的含义，其是组织蛋白酶K的抑制剂，并且可用于药物治疗用于治疗组织蛋白酶K的疾病和医学病症。各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症和肿瘤。

8. 发明申请

US20080027060A1 DIPEPTIDE NITRILES 审中-公开
标题翻译：西酞普兰
公开(公告)号：US20080027060A1
公开(公告)日：2008-01-31
申请号：US11835134
申请日：2007-08-07
申请人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Cowen , Paul Greenspan , Leslie McQuire , Ruben Tommasi , John van Duzer
发明人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Cowen , Paul Greenspan , Leslie McQuire , Ruben Tommasi , John van Duzer
IPC分类号： A61K31/404 , A61K31/166 , A61K31/341 , A61K31/415 , A61K31/495 , A61P19/02 , A61P29/00 , C07D207/09 , C07D209/08 , C07D333/24 , C07D307/54 , C07D295/14 , C07D295/04 , C07D231/12 , C07D213/56 , C07D207/33 , C07C233/64 , A61P19/10 , A61K31/5375 , A61K31/44 , A61K31/381 , A61K31/40
CPC分类号： C07C255/29 , C07C255/44 , C07C271/22 , C07C317/44 , C07C323/52 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D207/327 , C07D209/18 , C07D209/42 , C07D211/06 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/64 , C07D241/44 , C07D249/06 , C07D261/18 , C07D275/02 , C07D295/088 , C07D295/15 , C07D295/155 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/85 , C07D317/68 , C07D333/24 , C07D333/38 , C07D333/40 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06043 , C07K5/06078
摘要： N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
摘要翻译：定义的N-末端取代的二肽腈可用作半胱氨酸组织蛋白酶的抑制剂，例如，组织蛋白酶B，K，L和S，可用于治疗半胱氨酸组织蛋白酶依赖性疾病和病症，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症，肿瘤（特别是肿瘤侵袭和肿瘤转移），冠状动脉疾病，动脉粥样硬化（包括动脉粥样硬化斑块破裂和不稳定）。特别的二肽腈是式I化合物或生理上可接受的和可切割的酯或其盐，其中符号如上所定义。特别地，已经发现通过适当选择基团R 1，R 2，R 3，R 4，R 5， / SUB>，X 1，Y和L，化合物作为各种半胱氨酸组织蛋白酶类型的抑制剂的相对选择性，例如组织蛋白酶B，K，L和S可以被改变，例如，以获得选择性抑制特定组织蛋白酶类型或组织蛋白酶类型组合的抑制剂。

9. 发明申请

US20060142575A1 Hetereoaryl nitrile derivatives 失效
公开(公告)号：US20060142575A1
公开(公告)日：2006-06-29
申请号：US10525658
申请日：2003-08-29
申请人： Eva Altmann , Claudia Betschart , Kenji Hyakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
发明人： Eva Altmann , Claudia Betschart , Kenji Hyakawa , Osamu Irie , Junichi Sakaki , Genji Iwasaki , Rene Lattmann , Martin Missbach , Naoki Teno
IPC分类号： C07D473/02 , C07D239/72
CPC分类号： C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34
摘要： The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

10. 发明申请

US20090186889A1 SPIRO-SUBSTITUTED PYRROLOPYRIMIDINES 审中-公开
标题翻译：螺旋取代的吡咯烷酮
公开(公告)号：US20090186889A1
公开(公告)日：2009-07-23
申请号：US12413996
申请日：2009-03-30
申请人： Osamu Irie , Genji Iwasaki , Keiichi Masuya , Takahiro Miyake , Naoki Teno
发明人： Osamu Irie , Genji Iwasaki , Keiichi Masuya , Takahiro Miyake , Naoki Teno
IPC分类号： A61K31/5377 , C07D471/10 , A61K31/519
CPC分类号： C07D519/00
摘要： The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof formula I wherein the symbols have the meaning as defined in the description. Said compounds are inhibitors of cathepsin K and/or cathepsin S and are useful for the treatment of diseases and medical conditions in which cathepsin K and or cathepsin S is implicated, e.g. various disorders including neuropathic pain, inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, multiple sclerosis and tumours.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或其式I的化合物，其中符号具有如说明书中所定义的含义。所述化合物是组织蛋白酶K和/或组织蛋白酶S的抑制剂，并且可用于治疗涉及组织蛋白酶K和/或组织蛋白酶S的疾病和医学病症。各种疾病，包括神经性疼痛，炎症，类风湿性关节炎，骨关节炎，骨质疏松症，多发性硬化和肿瘤。

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