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1. 发明授权

US5686410A Polypeptide derivatives 失效
标题翻译：多肽衍生物
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。

2. 发明授权

US5656721A Peptide derivatives 失效
标题翻译：肽衍生物
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。

3. 发明授权

US5541159A Calcitonin derivatives 失效
标题翻译：降钙素衍生物
公开(公告)号：US5541159A
公开(公告)日：1996-07-30
申请号：US346118
申请日：1994-11-29
申请人： Rainer Albert , Wilfried Bauer , Fran.cedilla.ois Cardinaux , Janos Pless
发明人： Rainer Albert , Wilfried Bauer , Fran.cedilla.ois Cardinaux , Janos Pless
IPC分类号： A61K38/23 , A61K38/00 , A61K38/04 , A61P1/00 , A61P3/00 , A61P43/00 , C07K1/02 , C07K1/06 , C07K1/113 , C07K7/23 , C07K9/00 , C07K14/575 , C07K14/585 , A61K8/23
CPC分类号： C07K9/005 , C07K14/585 , C07K7/23 , C07K9/001 , A61K38/00
摘要： Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C.sub.3-5 alkyl attached to an amino group other than a N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos thati) when the calcitonin peptide comprises at least one sugar residue a), this sugar residue is attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.-amino substituted side chain in the 24 position, andii) when the LHRH antagonist comprises at least one sugar residue a), this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.-amino substituted side chain in the 8 positionin free form or in salt or complex form, have pharmacological activity.
摘要翻译：选自（i）由至少一种糖残基和/或至少一种短多羟基化合物或衍生物修饰的降钙素肽和LHRH拮抗剂肽的肽衍生物，和（ii）通过至少一种甲酰基和/或至少C3-5烷基连接到除了N-末端氨基以外的氨基，和（iii）通过所述取代基的组合修饰的降钙素肽，条件是i）当降钙素肽包含至少一个糖残基 a），该糖残基通过除了直接N-糖苷键之外的偶联与在24位的ω-氨基取代侧链的ω-氨基连接，和ii）当LHRH拮抗剂包含至少一种糖残基a），该糖残基是通过除直接N-糖苷键之外的偶联与游离形式的8位的ω-氨基取代侧链的ω-氨基或盐或复合物连接的阿马多糖残基形式，有p 有害活动。

4. 发明授权

US4496543A Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use 失效
标题翻译：多肽，其制备方法，包含所述多肽的药物组合物及其用途
公开(公告)号：US4496543A
公开(公告)日：1985-01-29
申请号：US524374
申请日：1983-08-18
申请人： Wilfried Bauer , Janos Pless
发明人： Wilfried Bauer , Janos Pless
IPC分类号： A61K38/00 , A61K38/04 , A61K38/27 , A61P1/00 , A61P1/04 , A61P3/08 , A61P3/10 , A61P5/00 , A61P9/00 , C07K7/06 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16 , Y10S930/26
摘要： Straight-chain or mono-cyclicpolypeptides comprising a heptapeptide moiety, said moiety having in the 1-position (N-terminal) an .alpha.-N-phenylalkylated, optionally ring-substituted phenylalanine residue, in the 2-position a cysteine residue, in the 3-position an optionally ring-substituted phenylalanine residue, in the 4-position an optionally benzene-ring-substituted tryptophan residue, in the 5-position an optionally .epsilon.-N-alkylated lysine residue and in the 7-position (C-terminal) a cysteine or cysteinol residue the S-atoms of the cysteine residue at the 2-position and the cysteine or cysteinol residue at the 7-position being linked together in the case of the mono-cyclic polypeptides to form an -S-S-bridge, whereby the residues at the 1-, 2-, 4-, 6-, and 7-positions of said heptapeptide moiety may each be in the (L)- or (D)-configuration and the residues at the 4-, 5- and 6-positions of said heptapeptide moiety may each be optionally .alpha.-N-alkylated, said polypeptides being in free or protected form, as well as salt forms and complexes thereof. Subject compounds are useful as pharmaceuticals, e.g. as GH-secretion inhibitors.
摘要翻译：包括七肽部分的直链或单环多肽，所述部分在2-位半胱氨酸残基中具有1-位（N-末端）α-N-烷基苯基烷基化，任选环取代的苯丙氨酸残基，在 3-位任选环取代的苯丙氨酸残基，在4-位任选的苯环取代的色氨酸残基，在5-位任选的ε-N-烷基化赖氨酸残基和7-位（C-末端）半胱氨酸或半胱氨酸残基，在2-位的半胱氨酸残基的S原子和7-位的半胱氨酸或半胱氨酸残基在单环多肽的情况下连接在一起以形成-SS桥，其中所述七肽部分的1-，2-，4-，6-和7-位上的残基可以各自为（L） - 或（D） - 构型，并且4-，5- 所述七肽部分的6-位可各自任选为α-烷基化的，所述多肽为游离或保护形式，以及其盐形式和复合物。主题化合物可用作药物，例如作为GH分泌抑制剂。

5. 发明授权

US4435385A N-Acyl-polypeptides and processes for the production thereof 失效
标题翻译： N-酰基多肽及其生产方法
公开(公告)号：US4435385A
公开(公告)日：1984-03-06
申请号：US353900
申请日：1982-03-02
申请人： Wilfried Bauer , Janos Pless
发明人： Wilfried Bauer , Janos Pless
IPC分类号： A61K38/00 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/26
摘要： N-Acyl-polypeptides comprising the basic sequence ##STR1## wherein "Acyl" is the acyl residue of an organic or inorganic acid; A is H or alkyl; >N--CH(Z)--CO-- and E are the residues of natural .alpha.-amino acids or corresponding (D)-amino acids; C is --Trp-- or --(D)Trp--; F is a terminal grouping; and Y.sub.1 and Y.sub.2 are each H or together are a direct bond; as well as their salt forms and complexes.
摘要翻译：包含碱基序列“IMAGE”的N-酰基多肽，其中“酰基”是有机或无机酸的酰基残基; A是H或烷基; > N-CH（Z）-CO-和E是天然α-氨基酸或相应的（D） - 氨基酸的残基; C是-Trp-或 - （D）Trp-; F是终端分组; Y1和Y2各自为H或一起为直接键; 以及它们的盐形式和复合物。

6. 发明授权

US4728638A Somatostatine derivatives 失效
标题翻译：生长激素衍生物
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。

7. 发明授权

US4261888A Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US4261888A
公开(公告)日：1981-04-14
申请号：US097630
申请日：1979-11-27
申请人： Wilfried Bauer , Francois Cardinaux , Rene Huguenin , Janos Pless , Edmond Sandrin
发明人： Wilfried Bauer , Francois Cardinaux , Rene Huguenin , Janos Pless , Edmond Sandrin
IPC分类号： C07K5/107 , C07C103/52
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention provides polypeptides of formula I,A-B-Gly-D-E Iwherein A is Tyr or substituted Tyr,B is -Gly- or -(D)Ala-,D is, for example, Phe or MePhe andE is, for example, -Met-X, -Leu-X, -Nle-X, -Nva-X, -Ile-X, methioninesulhoxide-X, methioninesulphone-X wherein X is --NR'R" or --OR'" and each of R', R" and R'" independently signifies hydrogen or alkyl of 1 to 5 carbon atoms,which compounds possess pharmacological activity, for example, analgesic activity.
摘要翻译：本发明提供了式I的多肽，其中A为Tyr或取代的Tyr，B为-Gly-或 - （D）Ala-，D为例如Phe或MePhe，E为例如AB-Gly-DE I ，-Met-X，-Leu-X，-Nle-X，-Nva-X，-Ile-X，甲硫氨酸 - X，甲硫氨酸 - X，其中X为-NR'R“或-OR” 的R'，R“和R”“独立地表示氢或1〜5个碳原子的烷基，该化合物具有药理活性，例如止痛活性。

8. 发明授权

US4438103A Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US4438103A
公开(公告)日：1984-03-20
申请号：US856617
申请日：1977-12-02
申请人： Wilfried Bauer , Francois Cardinaux , Rene Huguenin , Janos Pless , Edmond Sandrin
发明人： Wilfried Bauer , Francois Cardinaux , Rene Huguenin , Janos Pless , Edmond Sandrin
IPC分类号： C07D307/33 , A61K38/00 , A61P25/04 , A61P25/18 , C07C67/00 , C07C231/00 , C07C231/02 , C07K1/113 , C07K5/087 , C07K5/10 , C07K5/107 , C07K7/06 , C07K14/70 , A61K37/00 , C07C103/52
CPC分类号： C07K5/1016 , C07K14/702 , C07K5/0812 , A61K38/00 , Y10S514/80
摘要： The invention provides polypeptides of formula I,A--B--Gly--D--E IwhereinA is Tyr or substituted Tyr,B is --Gly-- or --(D)Ala--,D is, for example, Phe or MePheand E is, for example, --Met--X, --Leu--X,--Nle--X, --Nva--X, --Ile--X, methioninesulphoxide--X, methioninesulphone--X wherein X is --NR'R" or --OR'" and each of R', R" and R'" independently signifies hydrogen or alkyl of 1 to 5 carbon atoms,which compounds possess pharmacological activity, for example, analgesic activity.
摘要翻译：本发明提供了式I的多肽，其中A为Tyr或取代的Tyr，B为-Gly-或 - （D）Ala-，D为例如Phe或MePhe，E为例如AB-Gly-DE I ，-Met-X，-Leu-X，-Nle-X，-Nva-X，-Ile-X，甲硫氨酸氧化物-X，甲硫氨酸 - X，其中X为-NR'R“或-OR” 的R'，R“和R”“独立地表示氢或1〜5个碳原子的烷基，该化合物具有药理活性，例如止痛活性。

9. 发明授权

US4120852A Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US4120852A
公开(公告)日：1978-10-17
申请号：US575156
申请日：1975-05-07
申请人： Wilfried Bauer , Janos Pless
发明人： Wilfried Bauer , Janos Pless
IPC分类号： C07K7/08 , A61K38/00 , C07K14/575 , C07K14/655 , C07C103/52 , A61K37/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/26
摘要： This invention provides new compounds of formula I, ##STR1## wherein X is H-Ala, D-Ala, .beta.-Ala, propionyl or Ac-Ala (wherein Ac is pharmaceutically acceptable acyl),Y is hydrogen or a direct bond between the sulphur atoms in positions 3 and 14, andZ is the radical --COOH, --COOR.sub.1 (wherein R.sub.1 is lower alkyl), ##STR2## (wherein R.sub.2 and R.sub.3 independently are hydrogen or lower alkyl) or --CH.sub.2 OH,with the proviso that X is other than H-Ala, when Z is COOH.useful as agents for the treatment of Diabetes Mellitus, acromegaly and angiopathy.
摘要翻译：本发明提供了新的式I化合物，其中X为H-Ala，D-Ala，β-Ala，丙酰或Ac-Ala（其中Ac为药学上可接受的酰基），Y为氢或位置3和14之间的硫原子之间的直接键，Z是基团-COOH，-COOR1（其中R1是低级烷基），其中R2和R3独立地是氢或低级烷基或-CH2OH，与条件是X不是H-Ala，当Z是COOH时。

10. 发明授权

US4395403A Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use 失效
标题翻译：新型多肽，其制备方法，包含所述多肽的药物组合物及其用途
公开(公告)号：US4395403A
公开(公告)日：1983-07-26
申请号：US321663
申请日：1981-11-16
申请人： Wilfried Bauer , Janos Pless
发明人： Wilfried Bauer , Janos Pless
IPC分类号： C07K7/06 , A61K38/00 , A61K38/22 , A61P1/00 , A61P5/00 , C07C231/00 , C07K1/113 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/26
摘要： Straight-chain and mono-cyclic polypeptides containing the basic sequence ##STR1## wherein X is an amino acid residue, the residues in the 1- and 6-positions being linked by an --S--S-- bridge when the polypeptide is monocyclic, have pharmacological, in particular GH--, gastric- and pancreatic-secretion inhibiting activity.
摘要翻译：含有碱基序列“IMAGE”的直链和单环多肽，其中X为氨基酸残基，当多肽为单环时，通过-SS-桥连接的1位和6位的残基具有药理学，特别是GH-，胃和胰腺分泌抑制活性。

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