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    • 2. 发明授权
    • Peptides and processes for the manufacture thereof
    • 肽及其制造方法
    • US4316890A
    • 1982-02-23
    • US129066
    • 1980-03-10
    • Bruno KamberHans RinkPeter Sieber
    • Bruno KamberHans RinkPeter Sieber
    • C07K14/575A61K38/00A61K38/04A61P5/00A61P5/02C07K1/113C07K14/655A61K37/00C07C103/52
    • C07K14/6555A61K38/00Y10S930/16
    • The somatostatin-analogous peptides according to the invention of the general formula ##STR1## in which Bmp represents the desaminocysteine radicalX represents Asn or His,trp represents D-Trp that may be substituted in the benzene ring by a halogen atom, andY represents the radical of a secondary .alpha.-amino acid having a maximum of 8 carbon atomsand the corresponding peptide amides and also acid addition salts and complexes thereof are distinguished by strong insulin-antagonistic and glucagon-antagonistic effects and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially also as antidiabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates and by the formation of the cystine disulphide bridge by means of oxidation.
    • 根据本发明的通式(IMAGE)的生长抑素类似物肽,其中Bmp表示脱氨基半胱氨酸基团X表示Asn或His,trp表示可在苯环中被卤素原子取代的D-Trp,Y表示 具有最多8个碳原子的次级α-氨基酸的基团和相应的肽酰胺及其酸加成盐和复合物的特征在于强的胰岛素拮抗作用和胰高血糖素拮抗作用,并且因此是治疗上可接受的,优选在 形式的药物制剂,类似于生长抑素的适应症,特别是抗糖尿病药。 该化合物通过肽合成的常规方法制备,特别是通过相应的受保护的中间体的释放和通过氧化形成胱氨酸二硫桥。
    • 3. 发明授权
    • Novel cyclopeptides
    • 新型环肽
    • US4238481A
    • 1980-12-09
    • US942565
    • 1978-09-15
    • Hans RinkBruno KamberPeter Sieber
    • Hans RinkBruno KamberPeter Sieber
    • A61K38/00A61K38/04A61K38/22A61P5/00A61P5/02A61P43/00C07K1/113C07K5/097C07K7/06C07K7/56C07K14/575C07K14/655A61K37/00C07C103/52
    • C07K5/0821C07K14/6555A61K38/00Y02P20/55Y10S514/806Y10S930/16
    • Sulphur-free cyclopeptides with somatostatin-analogous aminoacid partial sequences, of the formula ##STR1## in which R is Asn, Ala or de-R, trp is D-Trp or L-Trp, which can be substituted in the benzene ring by halogen atoms or nitro groups, W is a free or etherified hydroxyl group or halogen atom present as a substituent on the benzene ring of the L-phenylalanine radical, or is hydrogen, X is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-X and Y is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-Y, and also acid addition salts and complexes thereof have biological properties similar to those of somatostatin and can be used, especially in the form of pharmaceutical preparations, for the treatment of excessive secretion of somatotropin, insulin and/or glucagon. The compounds according to the invention are obtained by cyclising a corresponding linear peptide compound in which the .epsilon.-amino group of the lysine radical and, if desired, also the hydroxyl group of the threonine radical are protected and detaching the protective groups which are present.
    • 具有生长抑素 - 类似氨基酸部分序列的无硫环肽,其中R为Asn,Ala或de-R,trp为式(I),其为可在苯中取代的D-Trp或L-Trp 卤素原子或硝基,W是在L-苯丙氨酸基团的苯环上作为取代基存在的游离的或醚化的羟基或卤素原子,或是氢,X是ω-氨基 - 低级烷烃的基团 - (单或二) - 羧酸或脱-X,Y是ω-氨基 - 低级烷烃 - (单或二) - 羧酸或脱Y的基团,并且其酸加成盐和络合物具有生物 特性与生长抑素相似,可用于治疗生长激素,胰岛素和/或胰高血糖素过度分泌的药物制剂形式。 根据本发明的化合物是通过环化相应的线性肽化合物而获得的,其中赖氨酸基团的ε-氨基和如果需要也保护苏氨酸基团的羟基并分离存在的保护基团。
    • 5. 发明授权
    • Cyclooctapeptides
    • 环肽
    • US4358439A
    • 1982-11-09
    • US216353
    • 1980-12-15
    • Peter SieberBruno KamberHans Rink
    • Peter SieberBruno KamberHans Rink
    • C07K7/56A61K38/00A61K38/04A61P5/00A61P5/02C07K1/113C07K14/575C07K14/655A61K37/00C07C103/52
    • C07K14/6555A61K38/00Y10S514/806Y10S930/16
    • Cyclic peptides of the formula ##STR1## in which trp represents L-Trp, D-Trp, or an analogous radical which carries a halogen atom in the indole nucleus, Ac.sub.A represents hydrogen, or an acyl radical Ac of a carboxylic acid present at the .epsilon.-amino group, A represents L-Phe, D-Phe, L-Phg or D-Phg, or a corresponding radical having a substituted or saturated phenyl ring, and B represents the residue of a .gamma.- or .delta.-amino-lower alkanecarboxylic acid which may carry an optionally substituted cyclic hydrocarbyl radical Ar, and also pharmacologically tolerable salts and therapeutically acceptable complexes thereof can be used as an antidiabetic in an analogous manner to somatostatin. They can be obtained by conventional processes of peptide chemistry, especially by cyclisation of corresponding linear peptides.
    • 其中trp表示L-Trp,D-Trp或在吲哚核中携带卤素原子的类似基团的式(I)的环肽,AcA表示氢或羧酸的酰基Ac 存在于ε-氨基,A表示L-Phe,D-Phe,L-Phg或D-Phg或具有取代或饱和的苯环的相应基团,B表示γ或δ- 可以携带任选取代的环状烃基Ar的氨基 - 低级链烷羧酸,以及其药理学上可耐受的盐和其可治疗可接受的复合物可以以与生长抑素类似的方式用作抗糖尿病剂。 它们可以通过肽化学的常规方法获得,特别是通过相应的线性肽的环化获得。
    • 8. 发明授权
    • Compositions of somatostatin analogues
    • 生长抑素类似物的组成
    • US07192570B2
    • 2007-03-20
    • US10486310
    • 2002-08-07
    • Helmut Robert MaeckeJean Claude ReubiHans RinkKlaus-Peter Eisenwiener
    • Helmut Robert MaeckeJean Claude ReubiHans RinkKlaus-Peter Eisenwiener
    • A61K38/12C07K14/655
    • A61K38/31C07K14/655
    • In one embodiment, a composition of somatostatin analogues having the general formula: is provided wherein Z may be absent or present and when present is selected from DOTA- and DTPA-based chelators, NOTA-based chelators, carbonyl compounds, hydrazino nicotinamide, N4-chelators, desferrioxamine, NxSy-chelators, optionally complexed or labeled with a radioisotope, tyrosine for halogenation, a fluorescent dye, or biotin. The composition further provides that L may or may not be present and when present is a linker molecule, X1 is glutamic acid or a symmetric or asymmetric diamino acid containing 3 or 4 consecutive C atoms, X2 is a positively charged natural or unnatural amino acid, an arginine mimic, citrulline, or a neutral amino acid, X3 is phenylalanine, Ala-[3-(2-thienyl)], α-naphthylalanine, or β-naphthylalanine, X4 is an aromatic amino acid, X5 is threonine or serine, and X6 is phenylalanine, Ala-[3-(2-thienyl)], α-naphthylalanine, or β-naphthylalanine.
    • 在一个实施方案中,提供了具有以下通式的生长抑素类似物的组合物:其中Z可以不存在或存在,并且当存在时选自DOTA-和DTPA-基螯合剂,NOTA-基螯合剂,羰基化合物,肼基烟酰胺, 切片,脱铁三胺,N x S x S - 切片,任选地用放射性同位素络合或标记,用于卤化的酪氨酸,荧光染料或 生物素。 该组合物还提供L可以存在或不存在,并且当存在连接分子时,X 1是谷氨酸或含有3或4个连续C原子的对称或不对称二氨基酸,X 2是带正电荷的天然或非天然氨基酸, 精氨酸模拟物,瓜氨酸或中性氨基酸,X3为苯丙氨酸,Ala- [3-(2-噻吩基)],α-萘丙氨酸或β-萘丙氨酸,X4为芳香族氨基酸,X5为苏氨酸或丝氨酸, 和X 6是苯丙氨酸,Ala- [3-(2-噻吩基)],α-萘基丙氨酸或β-萘基丙氨酸。