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1. 发明授权

US06953789B2 Thiol compounds, their production and use 失效
标题翻译：硫醇化合物，其生产和使用
公开(公告)号：US06953789B2
公开(公告)日：2005-10-11
申请号：US10757325
申请日：2004-01-13
申请人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
发明人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
IPC分类号： A61P19/02 , A61P19/10 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/76 , C07D211/78 , C07D211/88 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D223/10 , A61K31/4025 , A61K31/55 , C07D207/50
CPC分类号： C07D207/273 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/76 , C07D211/78 , C07D211/88 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc., each m may be same or different and is 0 or 1, n is an integer of 1 to 3, q1 is an integer of 1 to 2n+4, q2 is an integer of 0 to 2n+3, and the sum of q1 and q2 is 2n+4 or a salt thereof.
摘要翻译：本发明提供由下式表示的化合物：其中环A和环B可以相同或不同，并且各自为任选取代的杂环或杂环等，每个R 1可以相同或不同并且是氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2等，X 1是一个键，任选地取代的二价C 1-3 - 脂族烃基或-NR 3 - 等，X 2是一个键，任选取代的二价C < -SO 3 - 脂族烃基，-NR 4 - ， - O-或-S（O）p - （其中p为0,1）或2）中，每个Y可以相同或不同，为氢原子，任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR

2. 发明授权

US06699881B2 Thiol compounds, their production and use 失效
标题翻译：硫醇化合物，其生产和使用
公开(公告)号：US06699881B2
公开(公告)日：2004-03-02
申请号：US10161289
申请日：2002-06-03
申请人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
发明人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
IPC分类号： C07D21198
CPC分类号： C07D207/273 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/76 , C07D211/78 , C07D211/88 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc., each m may be same or different and is 0 or 1, n is an integer of 1 to 3, q1 is an integer of 1 to 2n+4, q2 is an integer of 0 to 2n+3, and the sum of q1 and q2 is 2n+4 or a salt thereof.
摘要翻译：本发明提供由下式表示的化合物：其中环A和环B可以相同或不同，并且各自为任选取代的杂环或杂环等，各R 1可以相同或不同，为氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2等，X 1是键，任选取代的二价C 1-3脂族烃基或-NR 3 - 等等，X 2是键，任选取代的二价C 1-3脂族烃基，-NR 4 - ， - O-或-S（O）p - （其中p是0,1或2）每个Y可以相同或不同，为氢原子，任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR 5，氧代基，硫代基，任选取代的亚氨基，硝基，氰基等，各m可以相同或不同，为0o r 1，n为1〜3的整数，q1为1〜2n + 4的整数，q2为0〜2n + 3的整数，q1和q2的和为2n +4或其盐。

3. 发明授权

US06420415B1 Thiol compounds, their production and use 失效
标题翻译：硫醇化合物，其生产和使用
公开(公告)号：US06420415B1
公开(公告)日：2002-07-16
申请号：US09787623
申请日：2001-03-20
申请人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
发明人： Toshiro Yamashita , Hiroshi Nara , Masayuki Takizawa , Koji Yoshimura
IPC分类号： C07D20750
CPC分类号： C07D207/273 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/76 , C07D211/78 , C07D211/88 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.
摘要翻译：由通式（1）表示的化合物或其盐具有基质金属蛋白酶抑制活性，可用作药物，其中环A和B各自表示任选取代的杂环或杂环等; R 1相同或不同，各自表示氢，任选取代的烃基，酰基等; X1表示键，任选取代的二价脂族烃基等; X 2表示键，任选取代的二价脂族烃基，-O-等; Y相同或不同，表示氢，任选取代的烃基，氧代等; m为0或1; n为1〜3的整数。 q1为1〜2n + 4的整数，并且q2为0〜2n + 3的整数，条件是q1 + q2为2n + 4。

4. 发明申请

US20050165064A1 Novel thiol derivative, process for producing the same and use thereof 审中-公开
标题翻译：新型硫醇衍生物，其制备方法及其用途
公开(公告)号：US20050165064A1
公开(公告)日：2005-07-28
申请号：US10512285
申请日：2003-04-24
申请人： Masahiro Kajino , Masayuki Takizawa , Kohei Notoya , Hiroshi Nara , Tomomi Ikemoto , Atsuko Nishiguchi
发明人： Masahiro Kajino , Masayuki Takizawa , Kohei Notoya , Hiroshi Nara , Tomomi Ikemoto , Atsuko Nishiguchi
IPC分类号： A61K31/4439 , A61P1/02 , A61P1/04 , A61P1/16 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D401/06 , C07D401/14 , C07D43/02
CPC分类号： C07D401/14 , A61K31/4439 , C07D401/06
摘要： The present invention provides a novel thiol derivative [I] which has an excellent matrix metalloprotease inhibiting activity and is useful as a pharmaceutical composition, particularly a therapeutic agent or prophylactic agent for osteoarthritis and rheumatoid arthritis and a salt thereof, the thiol derivative being a compound represented by the formula [I]: wherein ring A represents an optionally substituted aromatic heterocyclic ring; ring B represents an optionally substituted homocyclic or heterocyclic ring; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2 (wherein R2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group); X represents an optionally substituted divalent C1-3 aliphatic hydrocarbon group; Y represents an optionally substituted hydrocarbon group, a halogen atom, a carboxy group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR3 (wherein R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group), an oxo group, a thioxo group, an optionally substituted imino group, a nitro group or a cyano group; and q represents an integer of 0 to 5.
摘要翻译：本发明提供一种具有优异的基质金属蛋白酶抑制活性的新型硫醇衍生物[I]，可用作药物组合物，特别是用于骨关节炎和类风湿性关节炎的治疗剂或预防剂及其盐，硫醇衍生物为化合物由式[I]表示：其中环A表示任选取代的芳族杂环; 环B表示任选取代的杂环或杂环; R 1表示氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2（其中R 2，表示氢原子，任选取代的烃基，酰基或任选取代的杂环基）; X表示任选取代的二价C 1-3脂族烃基; Y表示任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR 3（其中R 3， SUP>表示氢原子，任选取代的烃基，酰基或任选取代的杂环基），氧代基，硫代基，任选取代的亚氨基，硝基或氰基; q表示0〜5的整数。

5. 发明授权

US06844546B2 Explosive detection system 有权
标题翻译：爆炸检测系统
公开(公告)号：US06844546B2
公开(公告)日：2005-01-18
申请号：US10229057
申请日：2002-08-28
申请人： Hisashi Nagano , Yasuaki Takada , Izumi Waki , Koushou Aikawa , Masayuki Takizawa , Shigenori Morishima
发明人： Hisashi Nagano , Yasuaki Takada , Izumi Waki , Koushou Aikawa , Masayuki Takizawa , Shigenori Morishima
IPC分类号： G01N27/62 , G01N1/22 , H01J49/00 , H01J49/04
CPC分类号： H01J49/0031
摘要： An explosive detection system including a sample injection region, an ion source region for generating ions of a sample injected by the ion injection region, a mass analysis region for analyzing mass of the ions, a heater for heating the sample injection region and the ion source region, a plurality of pumps for exhausting a chamber in which the mass analysis region is disposed, and a controller for controlling the regions and the plurality of pumps. The controller conducts control so as to heat the sample injection region and the ion source region with the heaters, then reduce heating electric power supplied to the heaters in order to prevent a predetermined electric power value from being exceeded, and drive the plurality of pumps successively to exhaust the chamber.
摘要翻译：一种爆炸检测系统，包括样品注入区域，用于产生由离子注入区域注入的样品的离子的离子源区域，用于分析离子质量的质量分析区域，用于加热样品注入区域的加热器和离子源区域，用于排出其中设置质量分析区域的室的多个泵，以及用于控制区域和多个泵的控制器。控制器进行控制，以便利用加热器加热样品注入区域和离子源区域，然后减少供给到加热器的加热电力，以防止超过预定的电功率值，并且依次驱动多个泵排气室。

6. 发明授权

US5716980A Alcohol or aldehyde derivatives and their use 失效
标题翻译：酒精或醛衍生物及其用途
公开(公告)号：US5716980A
公开(公告)日：1998-02-10
申请号：US495097
申请日：1995-06-27
申请人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
发明人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
IPC分类号： A61K38/55 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/27 , A61K38/00 , A61P3/00 , A61P3/02 , A61P43/00 , C07C231/12 , C07C233/18 , C07C233/22 , C07C233/31 , C07C237/10 , C07C237/22 , C07C271/16 , C07C271/18 , C07C271/22 , C07C303/40 , C07C311/19 , C07C337/02 , C07D209/14 , C07D209/16 , C07K1/113 , C07K5/06 , C07K5/062 , C07K14/81 , A61K31/40 , C07D209/20
CPC分类号： C07D209/16 , C07C233/18 , C07C233/22 , C07C233/31 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/19 , C07K5/06034 , A61K38/00 , Y02P20/55
摘要： The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof. Compound (I) is useful as a prophylactic/therapeutic agent for osteoporosis.
摘要翻译：本发明提供了含有下式化合物的组蛋白酶L抑制剂：其中R1是氢原子或可被取代的芳基烷基，杂环烷基或低级烷基; R2和R3独立地是氢原子或可以被取代的烃残基; R4是可以被取代的烷酰基，磺酰基，羰基氧基，氨基甲酰基或硫代氨基甲酰基; X是式：-CHO或-CHOOB（其中B是氢原子或羟基保护基）; m和n独立地为0或1的整数; 条件是R4是被芳基取代的烷酰基，被具有多于9个碳原子的芳基取代的磺酰基或低级烷基，或当R 1是未取代的低级烷基时可被取代的氨基甲酰基或硫代氨基甲酰基，甲基硫代乙基上的芳基烷基，R2和R3独立地是低级烷基或芳烷基，X是-CHO，m是1，n是0或1，或其盐。化合物（I）可用作骨质疏松症的预防/治疗剂。

7. 发明授权

US5668128A Aziridine derivatives, their production and use 失效
标题翻译：氮丙啶衍生物，其生产和使用
公开(公告)号：US5668128A
公开(公告)日：1997-09-16
申请号：US513896
申请日：1995-09-05
申请人： Shigetoshi Tsubotani , Masayuki Takizawa , Mikio Shirasaki , Junji Mizoguchi , Yoshiaki Shimizu
发明人： Shigetoshi Tsubotani , Masayuki Takizawa , Mikio Shirasaki , Junji Mizoguchi , Yoshiaki Shimizu
IPC分类号： A61K38/00 , C07D203/08 , C07D203/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/02 , C07K5/078 , C07D203/16 , A61K31/33 , A61K31/535 , C07D413/00
CPC分类号： C07D203/08 , C07D203/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/0222 , C07K5/06139 , A61K38/00
摘要： The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 and Q are independently an optionally esterified or amidated carboxyl group; R.sub.2 is hydrogen, an acyl group or an optionally substituted hydrocarbon residue; X is a divalent hydrocarbon residue which may be substituted; or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as agents for inhibiting thiol protease.
摘要翻译： PCT No.PCT / JP95 / 00718 Sec。 371 1995年9月5日第 102（e）1995年9月5日PCT PCT 1995年4月12日提交PCT公布。 WO95 / 28416 PCT出版物日期：1995年10月26日本发明涉及下式的化合物：其中R 1和Q独立地是任选酯化或酰胺化的羧基; R2是氢，酰基或任选取代的烃残基; X是可以被取代的二价烃残基; 或其盐，其可用作骨疾病的预防和治疗剂以及用作抑制硫醇蛋白酶的试剂。

8. 发明授权

US5639781A Alcohol or aldehyde derivatives and their use 失效
标题翻译：酒精或醛衍生物及其用途
公开(公告)号：US5639781A
公开(公告)日：1997-06-17
申请号：US495814
申请日：1995-06-27
申请人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
发明人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
IPC分类号： A61K38/55 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/27 , A61K38/00 , A61P3/00 , A61P3/02 , A61P43/00 , C07C231/12 , C07C233/18 , C07C233/22 , C07C233/31 , C07C237/10 , C07C237/22 , C07C271/16 , C07C271/18 , C07C271/22 , C07C303/40 , C07C311/19 , C07C337/02 , C07D209/14 , C07D209/16 , C07K1/113 , C07K5/06 , C07K5/062 , C07K14/81 , A61K31/40 , C07D209/08
CPC分类号： C07D209/16 , C07C233/18 , C07C233/22 , C07C233/31 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/19 , C07K5/06034 , A61K38/00 , Y02P20/55
摘要： The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Compound (I) is useful as a prophylactic/therapeutic agent for osteoporosis.
摘要翻译：本发明提供了含有下式化合物的组蛋白酶L抑制剂：其中R1是氢原子或可被取代的芳基烷基，杂环烷基或低级烷基; R2和R3独立地是氢原子或可以被取代的烃残基; R4是可以被取代的烷酰基，磺酰基，羰基氧基，氨基甲酰基或硫代氨基甲酰基; X是式：-CHO或-CHOOB（其中B是氢原子或羟基保护基）; m和n独立地为0或1的整数; 条件是R4是被芳基取代的烷酰基，被具有多于9个碳原子的芳基取代的磺酰基或低级烷基，或当R 1是未取代的低级烷基时可被取代的氨基甲酰基或硫代氨基甲酰基，甲基硫代乙基上的芳基烷基，R2和R3独立地是低级烷基或芳烷基，X是-CHO，m是1，n是0或1，或其盐。化合物（I）可用作骨质疏松症的预防/治疗剂。

9. 发明申请

US20060034832A1 Cell death inhibitor 审中-公开
标题翻译：细胞死亡抑制剂
公开(公告)号：US20060034832A1
公开(公告)日：2006-02-16
申请号：US10512587
申请日：2003-04-24
申请人： Haruhide Kimura , Yoshimi Sato , Masayuki Takizawa , Takashi Horiguchi , Kohei Notoya
发明人： Haruhide Kimura , Yoshimi Sato , Masayuki Takizawa , Takashi Horiguchi , Kohei Notoya
IPC分类号： A61K39/395 , A61K31/5415
CPC分类号： C07D417/04 , A61K31/00 , A61K31/5415 , C07D279/08 , G01N2333/52 , G01N2500/02
摘要： The cell death inhibitor comprising a substance capable of binding to macrophage migration inhibitory factor is useful as a preventive/therapeutic agent for, e.g., heart diseases, neurodegenerative diseases, cerebrovascular diseases, central nervous infections, traumatic diseases, demyelinating diseases, bone/joint diseases, kidney diseases, liver diseases, myelodysplastic diseases, arteriosclerosis, diabetes, pulmonary hypertension, sepsis, inflammatory bowel diseases, autoimmune diseases, failure accompanying rejection in organ transplantation, AIDS, cancer, etc.
摘要翻译：包含能够结合巨噬细胞迁移抑制因子的物质的细胞死亡抑制剂可用作例如心脏病，神经变性疾病，脑血管疾病，中枢神经感染，创伤性疾病，脱髓鞘疾病，骨/关节疾病的预防/治疗剂肾脏疾病，肝脏疾病，骨髓增生异常性疾病，动脉硬化，糖尿病，肺动脉高压，败血症，炎症性肠病，自身免疫疾病，器官移植排斥反应失败，艾滋病，癌症等。

10. 发明授权

US5679708A Epoxysuccinic acid derivatives, their production and use 失效
标题翻译：环氧琥珀酸衍生物，其生产和使用
公开(公告)号：US5679708A
公开(公告)日：1997-10-21
申请号：US513895
申请日：1995-09-05
申请人： Shigetoshi Tsubotani , Masayuki Takizawa , Junji Mizoguchi
发明人： Shigetoshi Tsubotani , Masayuki Takizawa , Junji Mizoguchi
IPC分类号： C07D303/48 , A61K31/335 , C07D405/12
CPC分类号： C07D303/48
摘要： The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 stands for an optionally esterified or amidated carboxyl group, X stands for an optionally substituted divalent hydrocarbon residue, R.sub.2 stands for hydrogen or an optionally substituted hydrocarbon residue, R.sub.3 stands for an alkyl group which is substituted with a group bonded through O or S(O).sub.n wherein n is 0, 1 or 2, with a proviso that when the partial structural formula: --NH--X--CO-- is leucine residue, R.sub.3 is not 3-hydroxy-3-methylbutyl group nor 4-hydroxy-3-methylbutyl group, or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as inhibitory agents of thiol protease.
摘要翻译： PCT No.PCT / JP95 / 01004 Sec。 371 1995年9月5日第 102（e）1995年9月5日PCT PCT 1995年5月25日PCT公布。出版物WO95 / 32954 日期：1994年12月7日本发明涉及下式化合物：其中R1代表任意酯化或酰胺化的羧基，X代表任意取代的二价烃残基，R2代表氢或任选取代的烃基，R3代表被O或S（O）n键合的基团取代的烷基，其中n为0,1或2，条件是当部分结构式为：-NH-X- CO-是亮氨酸残基，R3不是3-羟基-3-甲基丁基也不是4-羟基-3-甲基丁基，或其盐，其可用作骨疾病的预防和治疗剂，并且作为硫醇蛋白酶的抑制剂。

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