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公开(公告)号：EP0679659A1
公开(公告)日：1995-11-02
申请号：EP94931695.4
申请日：1994-11-08
发明人： KATSUNUMA, Nobuhiko , TURK, Vito
CPC分类号： C07K14/8139 , A61K38/00
摘要： A polypeptide having the amino acid sequence represented by the following SEQ ID NO: 1, and a cathepsin-L-specific inhibitor and an osteoporosis remedy each containing the polypeptide as the active ingredient. The polypeptide has such potent cathepsin-L-specific inhibitor and bone resorption inhibitor activities that it is useful for treating osteoporoses, in particular, senile osteoporosis.
摘要翻译： 具有由下列SEQ ID NO：1表示的氨基酸序列的多肽和组织蛋白酶-L特异性抑制剂和各自含有多肽作为活性成分的骨质疏松症药物。 该多肽具有这样有效的组织蛋白酶-L特异性抑制剂和骨吸收抑制剂活性，其用于治疗骨质疏松症，特别是老年性骨质疏松症。
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公开(公告)号：EP0822260B1
公开(公告)日：2004-01-21
申请号：EP97904590.3
申请日：1997-02-20
发明人： KITANO, Shizuo , SASAKI, Toru , YOSHIDA, Kenichiro , OTANI, Toshio , YU, Lei , WU, Yun , KATSUNUMA, Nobuhiko
CPC分类号： C07K5/06095 , A61K38/00 , C12P21/02
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公开(公告)号：EP0679659B1
公开(公告)日：1999-04-14
申请号：EP94931695.4
申请日：1994-11-08
发明人： KATSUNUMA, Nobuhiko , TURK, Vito
CPC分类号： C07K14/8139 , A61K38/00
摘要： A polypeptide having the amino acid sequence represented by the following SEQ ID NO: 1, and a cathepsin-L-specific inhibitor and an osteoporosis remedy each containing the polypeptide as the active ingredient. The polypeptide has such potent cathepsin-L-specific inhibitor and bone resorption inhibitor activities that it is useful for treating osteoporoses, in particular, senile osteoporosis.
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4.发明公开EPOXYSUCCINAMIDE DERIVATIVES OR SALTS THEREOF, AND DRUGS CONTAINING THE SAME 失效EPOXYSUCCINAMID-DERIVATE ODER DENEN SALZE UND MEDIKAMENTE DIEE ENTHALTEN
公开(公告)号：EP0808839A1
公开(公告)日：1997-11-26
申请号：EP96941212.1
申请日：1996-12-10
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by the general formula (1)
wherein R 1 and R 2 are the same or different from each other and independently represent H or an aromatic hydrocarbon group or aralkyl group which may be substituted, or R 1 and R 2 may form a nitrogen-containing heterocyclic ring together with the adjacent nitrogen atoms, R 3 is H or an acyl group, R 4 is H or an aralkyl group, and R 5 is an aromatic hydrocarbon group or aralkyl group which may be substituted, or R 5 may form an amino acid residue, which may be protected, together with the adjacent nitrogen atom, or a salt thereof, and a medicine comprising the derivative as an active ingredient.
This compound has an inhibiting activity against cathepsin, and particularly, specifically inhibits cathepsin L and is hence useful for prevention and treatment of osteopathy such as osteoporosis.摘要翻译： 本发明涉及由通式（1）
表示的环氧琥珀酰胺衍生物，其中R 1和R 2彼此相同或不同，并且独立地表示H或芳族烃基或芳烷基，其可以是 或R 1和R 2可以与相邻的氮原子一起形成含氮杂环，R 3是H或酰基，R 4是H或芳烷基，和 R 5是可以被取代的芳族烃基或芳烷基，或者可以与相邻的氮原子或其盐一起形成可以被保护的氨基酸残基，或者包含 该衍生物作为活性成分。 该化合物对组织蛋白酶具有抑制作用，特别是抑制组织蛋白酶L，因此可用于预防和治疗骨质疏松症等骨病。 -
5.发明授权EPOXYSUCCINAMIDE DERIVATIVES OR SALTS THEREOF, AND DRUGS CONTAINING THE SAME 失效环氧琥珀衍生物或它们的盐及药物含有它们的
公开(公告)号：EP0808839B1
公开(公告)日：2001-05-23
申请号：EP96941212.1
申请日：1996-12-10
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： Epoxysuccinamide derivatives represented by general formula (1) or salts thereof and drugs comprising the same as the active ingredient, wherein R?1 and R2¿ are the same or different and each represents H or optionally substituted aromatic hydrocarbyl or aralkyl, or R?1 and R2¿ may form a nitrogenous heterocycle in cooperation with the adjacent nitrogen atom; R3 represents H or acyl; R4 represents H or aralkyl; and R5 represents optionally substituted aromatic hydrocarbyl or aralkyl or may form an optionally protected amino acid residue in cooperation with the adjacent nitrogen atom. These compounds have a cathepsin inhibitory activity, in particular a specific inhibitory activity against cathepsin L, and are hence effective in the prophylaxis and therapy of bone diseases such as osteoporosis.
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6.发明公开SUBSTANCE FA-70D, PROCESS FOR PRODUCING THE SAME, AND USES THEREOF 失效SUBSTANZ FA-70D，HERSTELLUNGSVERFAHREN UND VERWENDUNGEN
公开(公告)号：EP0822260A1
公开(公告)日：1998-02-04
申请号：EP97904590.3
申请日：1997-02-20
发明人： KITANO, Shizuo , SASAKI, Toru , YOSHIDA, Kenichiro , OTANI, Toshio , YU, Lei , WU, Yun , KATSUNUMA, Nobuhiko
CPC分类号： C07K5/06095 , A61K38/00 , C12P21/02
摘要： Substance FA-70D which has the following formula (1) or its salt, a method for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating osteoporosis which comprises administering the compound, use of the compound as a drug, and a microorganism capable of producing Substance FA-70D.
This compound has specific inhibitory activity against cathepsin series proteases and is of value as a therapeutic drug for various diseases with which these enzymes are associated, particularly osteoporosis.摘要翻译： 具有下式（1）的物质FA-70D或其盐，其制备方法，包含该化合物作为活性成分的药物组合物，治疗骨质疏松症的方法，其包括施用该化合物，使用该化合物作为 药物和能够产生物质FA-70D的微生物。
该化合物对组织蛋白酶系列蛋白酶具有特异性抑制活性，作为与这些酶相关的各种疾病，特别是骨质疏松症的治疗药物是有价值的。
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