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公开(公告)号:US20110172157A1
公开(公告)日:2011-07-14
申请号:US13048932
申请日:2011-03-16
申请人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
发明人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
CPC分类号: C07K7/64 , A61K38/00 , C07K14/655 , Y02P20/55
摘要: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
摘要翻译: 本发明提供任选以保护形式的环[{4-(NH 2 -C 2 H 4 -NH-CO-O-)Pro} -Phg-DTrp-Lys-Tyr(4-苄基)-Phe]或其药学上可接受的盐或 其复合物,其具有有趣的药物性质。
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公开(公告)号:US07473761B2
公开(公告)日:2009-01-06
申请号:US10343288
申请日:2001-07-30
申请人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
发明人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
IPC分类号: C07K7/64
CPC分类号: C07K7/64 , A61K38/00 , C07K14/655 , Y02P20/55
摘要: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
摘要翻译: 本发明提供任选以保护形式的环[{4-(NH 2 -C 2 H 4 -NH-CO-O-)Pro} -Phg-DTrp-Lys-Tyr(4-苄基)-Phe]或其药学上可接受的盐或 其复合物,其具有有趣的药物性质。
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公开(公告)号:US20050009147A1
公开(公告)日:2005-01-13
申请号:US10848279
申请日:2004-05-18
申请人: Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
发明人: Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
IPC分类号: C07K9/00 , A61K38/00 , A61K38/22 , A61K38/29 , A61P3/00 , A61P3/14 , A61P19/08 , A61P43/00 , C07K20060101 , C07K14/01 , C07K14/195 , C07K14/41 , C07K14/635 , C07K19/00 , C12N1/20 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/16 , C12N15/62 , C12P21/02 , C12R1/19 , C07H21/04
CPC分类号: C07K14/005 , A61K38/00 , C07K14/635 , C07K2319/00 , C07K2319/50 , C07K2319/75 , C12N2795/10222
摘要: PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
摘要翻译: 具有PTH样活性并且包含至少一个修饰的PTH化合物,所述修饰是1.至少一个选自L-或D-α-氨基酸,C2-6羰基和任选取代的C 1-8烷基的基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的末端氨基,和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的一个或多个侧链氨基,或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代,由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代,或 这些修改的组合,免费的 m或盐形式,具有药理活性,例如。 用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。
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公开(公告)号:US5656721A
公开(公告)日:1997-08-12
申请号:US272704
申请日:1994-07-07
申请人: Rainer Albert , Wilfried Bauer , Francois Cardinaux , Monika Mergler , Janos Pless , Walter Prikoszovich
发明人: Rainer Albert , Wilfried Bauer , Francois Cardinaux , Monika Mergler , Janos Pless , Walter Prikoszovich
IPC分类号: A61K31/70 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/43 , A61K38/55 , A61P1/00 , A61P1/04 , A61P3/08 , A61P5/00 , A61P9/00 , C07K1/00 , C07K1/02 , C07K1/107 , C07K1/113 , C07K1/12 , C07K7/06 , C07K7/16 , C07K9/00 , C07K14/00 , C07K14/52 , C07K14/575 , C07K14/585 , C07K14/60 , C07K14/62 , C07K14/655 , C07K17/08 , A61K38/31
CPC分类号: C07K9/00 , C07K1/1077 , Y02P20/55
摘要: The present invention provides a sugar derivative of a biologically active peptide, which derivative has a prolonged duration of action when compared to the non-sugar modified peptide, and contains at least on one of the amino acid units a sugar residue which is attached to an amino group thereof by a coupling other than a direct N-glycosidic bond, and additionally, when it is a condensation product of a carboxyl group containing sugar and a peptide with less than 8 amino acid units, by a coupling other than a direct amide bond.
摘要翻译: 本发明提供了一种生物活性肽的糖衍生物,该衍生物与非糖修饰肽相比具有延长的作用时间,并且在至少一个氨基酸单元上含有连接到 通过除直接N-糖苷键以外的偶联的氨基,此外,当它是含羧基的糖和小于8个氨基酸单元的肽的缩合产物时,通过除直接酰胺键之外的偶联 。
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公开(公告)号:US07939625B2
公开(公告)日:2011-05-10
申请号:US12265135
申请日:2008-11-05
申请人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
发明人: Rainer Albert , Wilfried Bauer , David Bodmer , Christian Bruns , Ivo Felner , Heribert Hellstern , Ian Lewis , Mark Meisenbach , Gisbert Weckbecker , Bernhard Wietfeld
IPC分类号: C07K7/64
CPC分类号: C07K7/64 , A61K38/00 , C07K14/655 , Y02P20/55
摘要: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
摘要翻译: 本发明提供任选以保护形式的环[{4-(NH 2 -C 2 H 4 -NH-CO-O-)Pro} -Phg-DTrp-Lys-Tyr(4-苄基)-Phe]或其药学上可接受的盐或 其复合物,其具有有趣的药物性质。
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公开(公告)号:US20080318838A1
公开(公告)日:2008-12-25
申请号:US12169134
申请日:2008-07-08
申请人: Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
发明人: Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
CPC分类号: C07K14/005 , A61K38/00 , C07K14/635 , C07K2319/00 , C07K2319/50 , C07K2319/75 , C12N2795/10222
摘要: PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
摘要翻译: 具有PTH样活性并且包含至少一个修饰的PTH化合物,所述修饰是1.至少一个选自L-或D-α-氨基酸,C2-6羰基和任选取代的C 1-8烷基的基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的末端氨基,和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的一个或多个侧链氨基,或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代,由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代,或 这些修改的组合,免费的 m或盐形式,具有药理活性,例如。 用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。
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公开(公告)号:US06818638B2
公开(公告)日:2004-11-16
申请号:US10192888
申请日:2002-07-11
申请人: Rolf Baenteli , Wilfried Bauer , Sylvain Cottens , Claus Ehrhardt , Ulrich Hommel , Jörg Kallen , Josef Gottfried Meingassner , François Nuninger , Gabriele Weitz Schmidt
发明人: Rolf Baenteli , Wilfried Bauer , Sylvain Cottens , Claus Ehrhardt , Ulrich Hommel , Jörg Kallen , Josef Gottfried Meingassner , François Nuninger , Gabriele Weitz Schmidt
IPC分类号: A61K3133
CPC分类号: C07C271/12 , C07C235/26 , C07C235/30 , C07C237/18 , C07C2602/28 , C07D211/76 , C07D265/10
摘要: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
摘要翻译: 其中内酯环被修饰的美维林衍生物具有令人感兴趣的药物性质,特别是在预防或治疗由LFA-1 / ICAM-1相互作用介导的疾病或疾病中。
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公开(公告)号:US5686410A
公开(公告)日:1997-11-11
申请号:US276280
申请日:1994-07-18
申请人: Rainer Albert , Wilfried Bauer , Janos Pless
发明人: Rainer Albert , Wilfried Bauer , Janos Pless
IPC分类号: A61K47/48 , A61K51/08 , A61K38/18 , C07K14/485
CPC分类号: A61K47/48276 , A61K47/48238 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要: A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.
摘要翻译: 选自生长因子,肽激素,干扰素和细胞因子及其类似物和衍生物的生物活性肽,并且具有与所述肽的氨基连接的至少一个螯合基团,所述螯合基团能够络合可检测元件,并且所述氨基 与靶受体没有显着结合亲和力的基团与可检测元件复合并且可用作药物,例如, 用于靶组织的体内成像或用于治疗的放射性药物。
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公开(公告)号:US4728638A
公开(公告)日:1988-03-01
申请号:US816663
申请日:1986-01-07
申请人: Wilfried Bauer , Janos Pless , Rene Huguenin
发明人: Wilfried Bauer , Janos Pless , Rene Huguenin
IPC分类号: A61K38/00 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号: C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要: Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.
摘要翻译: 其中(a)A是-CO-N(A4)或-N(A5)-CO-,Y1和Y2是H或一起键或(b)的通式
的生长激素衍生物 )A是H,烷基,苯基烷基或RCO,Y 1和Y 2是如权利要求1中定义的酰基,A',B,C,D,E,F,A1,A2,A3,A4,A5,R和Z具有 权利要求1所述的含义具有药理学,特别是GH-,胃和胰腺分泌抑制活性。 -
公开(公告)号:US4291022A
公开(公告)日:1981-09-22
申请号:US152706
申请日:1980-05-23
申请人: Edmond Sandrin , Wilfried Bauer
发明人: Edmond Sandrin , Wilfried Bauer
IPC分类号: A61K38/00 , C07K5/083 , C07K5/103 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号: C07K14/6555 , C07K5/0808 , C07K5/1005 , A61K38/00 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要: This invention provides new compounds of formula I, ##STR1## wherein R.sub.1, X, Y and Z are amino acid residues andeach B is hyrogen or together are a bond,useful as growth hormone secretion inhibitors.
摘要翻译: 本发明提供了新的式I化合物,其中R1,X,Y和Z是氨基酸残基,每个B是氢或一起是可用作生长激素分泌抑制剂的键。
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