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1. 发明授权

US6110892A Parathyroid hormone analogues for the treatment of osteoporosis 失效
标题翻译：甲状旁腺素类似物用于治疗骨质疏松症
公开(公告)号：US6110892A
公开(公告)日：2000-08-29
申请号：US904760
申请日：1997-08-01
申请人： Jean-Rene Barbier , Paul Morley , Witold Neugebauer , Virginia J. S. Ross , James F. Whitfield , Gordon E. Willick
发明人： Jean-Rene Barbier , Paul Morley , Witold Neugebauer , Virginia J. S. Ross , James F. Whitfield , Gordon E. Willick
IPC分类号： A61K38/00 , C07K14/635 , A61K38/29
CPC分类号： A61K38/29 , C07K14/635
摘要： This invention describes analogues of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailabilities. The peptides described are derivatives of hPTH-(1-31) which are cyclized for example, by formation of lactams between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogues have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogues also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat. An assay which correlates hypotensive activity with osteogenic activity is also described.
摘要翻译：本发明描述了人甲状旁腺激素的类似物，其具有增加的骨修复活性和增加的生物利用度。所描述的肽是hPTH-（1-31）的衍生物，其被环化，例如通过在Glu22和Lys26或Lys26和Asp30之间形成内酰胺。此外，天然Lys27可以被Leu或其它疏水性残基例如Ile，正亮氨酸，Met，Val，Ala，Trp或Phe取代。通常，这些类似物具有增强的能力来刺激大鼠骨肉瘤细胞中的腺苷酸环化酶，并且使用卵巢切除的大鼠模型显示增加的骨修复活动。类似物还显示出增强的活性和生物利用度，如其在大鼠中的降血压作用所证明的。还描述了将降血压活性与成骨活性相关联的测定法。

2. 发明授权

US06541450B1 Parathyroid hormone analogues for the treatment of osteoporosis 失效
标题翻译：甲状旁腺素类似物用于治疗骨质疏松症
公开(公告)号：US06541450B1
公开(公告)日：2003-04-01
申请号：US09536785
申请日：2000-03-28
申请人： Jean-Rene Barbier , Paul Morley , Witold Neugebauer , James F. Whitfield , Gordon E. Willick
发明人： Jean-Rene Barbier , Paul Morley , Witold Neugebauer , James F. Whitfield , Gordon E. Willick
IPC分类号： A61K3829
CPC分类号： A61K38/29 , C07K14/635
摘要： This invention describes analogues of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailability. The peptides described are derivatives of hPTH-(1-31) which are cyclized for example, by formation of lactams between either Glu22 and Lys26 or Lys26 and Asp30. In addition, the natural Lys27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogues have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogues also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat. An assay which correlates hypotensive activity with osteogenic activity is also described.
摘要翻译：本发明描述了人甲状旁腺激素的类似物，其具有增加的骨修复活性和增加的生物利用度。所描述的肽是hPTH-（1-31）的衍生物，其被环化，例如通过在Glu22和Lys26或Lys26和Asp30之间形成内酰胺。此外，天然Lys27可以被Leu或其它疏水性残基例如Ile，正亮氨酸，Met，Val，Ala，Trp或Phe取代。通常，这些类似物具有增强的能力来刺激大鼠骨肉瘤细胞中的腺苷酸环化酶，并且使用卵巢切除的大鼠模型显示增加的骨修复活动。类似物还显示出增强的活性和生物利用度，如其在大鼠中的降血压作用所证明的。还描述了将降血压活性与成骨活性相关联的测定法。

3. 发明授权

US06316410B1 Parathyroid hormone analogues for the treatment of osteoporosis 有权
标题翻译：甲状旁腺素类似物用于治疗骨质疏松症
公开(公告)号：US06316410B1
公开(公告)日：2001-11-13
申请号：US09406813
申请日：1999-09-22
申请人： Jean-René Barbier , Paul Morley , James F. Whitfield , Gordon E. Willick
发明人： Jean-René Barbier , Paul Morley , James F. Whitfield , Gordon E. Willick
IPC分类号： A61K3800
CPC分类号： C07K14/635 , A61K38/00
摘要： The invention disclosed relates to analogues of human parathyroid hormoneh(PTH) which have increased activities in bone restoration, and increased bioavailablities. The analogues described are either single cyclic (1-28) or (1-29) analogues, or double cyclic (1-28) to (1-31) analogues. The single cyclic analogues are cyclised between amino acid pairs R22 and R26. The double cyclic analogues are cyclised between amino acid pairs 13 and 17, and 22 and 26. Various substitutions of the natural residues for other amino acids are also described. For example, the natural Lys27 residue may be substituted by Leu. Typically, these novel analogues have enhanced abilities to stimulate adenyl cyclase activity in rat osteosarcoma cells, and show increased activities in bone restoration using the ovariectomized rat model.
摘要翻译：所公开的发明涉及人甲状旁腺激素（PTH）的类似物，其具有增加的骨修复活性和增加的生物可利用性。所描述的类似物是单环（1-28）或（1-29）类似物，或双环（1-28）至（1-31）类似物。单个环状类似物在氨基酸对R22和R26之间环化。双环类似物在氨基酸对13和17之间以及22和26之间环化。还描述了其它氨基酸的天然残基的各种取代。例如，天然的Lys27残基可以被Leu取代。通常，这些新型类似物具有增强的刺激大鼠骨肉瘤细胞中腺苷酸环化酶活性的能力，并且使用卵巢切除的大鼠模型显示增加的骨修复活动。

4. 发明授权

US5955425A Parathyroid hormone analogues for the treatment of osteoporosis 失效
标题翻译：甲状旁腺素类似物用于治疗骨质疏松症
公开(公告)号：US5955425A
公开(公告)日：1999-09-21
申请号：US691647
申请日：1996-08-02
申请人： Paul Morley , Witold Neugebauer , Virginia J. S. Ross , James F. Whitfield , Gordon E. Willick , Jean-Rene Barbier
发明人： Paul Morley , Witold Neugebauer , Virginia J. S. Ross , James F. Whitfield , Gordon E. Willick , Jean-Rene Barbier
IPC分类号： A61K20060101 , A61K38/29 , C07H20060101 , C07J20060101 , C07K20060101 , C07K14/635
CPC分类号： C07K14/635 , A61K38/29
摘要： This invention describes analogs of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailabilities. The peptides described are derivatives of hPTH-(1-31) which have lactams formed for example, between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogs have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogs also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat.
摘要翻译：本发明描述了人甲状旁腺激素的类似物，其具有增加的骨修复活性和增加的生物利用度。描述的肽是hPTH-（1-31）的衍生物，其具有例如在Glu22和Lys26或Lys26和Asp30之间形成的内酰胺。此外，天然Lys27可以被Leu或其它疏水性残基例如Ile，正亮氨酸，Met，Val，Ala，Trp或Phe取代。通常，这些类似物具有增强在大鼠骨肉瘤细胞中刺激腺苷酸环化酶的能力，并且使用卵巢切除的大鼠模型显示增加的骨修复活动。类似物还显示出增强的活动和生物利用度，如其在大鼠中的降血压作用所证明的。

5. 发明授权

US5556940A Parathyroid hormone analogues for the treatment of osteoporosis 失效
标题翻译：甲状旁腺素类似物用于治疗骨质疏松症
公开(公告)号：US5556940A
公开(公告)日：1996-09-17
申请号：US262495
申请日：1994-06-20
申请人： Gordon E. Willick , James F. Whitfield , Witold Surewicz , Wing L. Sung , Witold Neugebauer
发明人： Gordon E. Willick , James F. Whitfield , Witold Surewicz , Wing L. Sung , Witold Neugebauer
IPC分类号： A61K38/00 , C07K14/635 , A61K38/29
CPC分类号： C07K14/635 , A61K38/00
摘要： Certain analogues of human parathyroid hormone (hPTH) have been found to be effective for the treatment of osteoporosis, while showing decreased side effects. Analogues showing this effect include all sequences from hPTH-(1-28)-NH.sub.2 to hPTH-(1-31)-NH.sub.2 and all sequences from [Leu.sup.27 ]-hPTH-(1-28)-NH.sub.2 to [Leu.sup.27 ]-hPTH-(1-33)-NH.sub.2. Also included are cyclic analogues cyclo(Lys.sup.26 -Asp.sup.30) [Leu.sup.27 ]-hPTH-(1-34)NH.sub.2 and cyclo (Lys.sup.27 -Asp.sup.30 )-hPTH-(1-34)-NH.sub.2. Analogues in the form of the carboxyl terminal amide are particularly effective.
摘要翻译：已经发现人类甲状旁腺激素（hPTH）的某些类似物对于治疗骨质疏松症是有效的，同时显示出副作用降低。显示该效应的类似物包括从hPTH-（1-28）-NH2至hPTH-（1-31）-NH2的所有序列，以及[Leu27] -hPTH-（1-28）-NH2至[Leu27] -hPTH - （1-33）-NH 2。还包括环状类似物环（Lys26-Asp30）[Leu27] -hPTH-（1-34）NH2和环（Lys27-Asp30）-hPTH-（1-34）-NH2。羧基末端酰胺形式的类似物是特别有效的。

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