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1. 发明授权

US06342373B1 Process for preparing recombinant eglin, protease inhibitor 失效
标题翻译：重组eglin，蛋白酶抑制剂的制备方法
公开(公告)号：US06342373B1
公开(公告)日：2002-01-29
申请号：US07707265
申请日：1991-05-24
申请人： Hans Rink , Manfred Liersch , Peter Sieber , Werner Rittel , Francois Meyer , Ursula Seemüller , Hans Fritz , Walter Märki , Sefik Alkan
发明人： Hans Rink , Manfred Liersch , Peter Sieber , Werner Rittel , Francois Meyer , Ursula Seemüller , Hans Fritz , Walter Märki , Sefik Alkan
IPC分类号： C12N1509
CPC分类号： C07K16/38 , A61K2039/505
摘要： The invention relates to DNA sequences which code an eglin, expression plasmids containing such DNA sequences, hosts transformed with such expression plasmids, novel eglin compounds produced from such transformed hosts, monoclonal antibodies against eglins, hybridoma cells which produce such antibodies, and test kits for immunoassays containing such antibodies, and furthermore the processes for their preparation and a process for the preparation of eglins with the aid of the transformed hosts. The eglins which can be prepared according to the invention have useful pharmacological properties.
摘要翻译：本发明涉及编码eglin的DNA序列，含有这样的DNA序列的表达质粒，用这种表达质粒转化的宿主，由这样的转化宿主产生的新的eglin化合物，产生此类抗体的杂交瘤细胞，含有此类抗体的免疫测定法，以及其制备方法以及借助于转化的宿主制备埃可林的方法。可根据本发明制备的胰蛋白酶具有有用的药理学性质。

2. 发明授权

US5728549A Process for the manufacture of thrombin inhibitors 失效
公开(公告)号：US5728549A
公开(公告)日：1998-03-17
申请号：US398416
申请日：1995-03-03
申请人： Manfred Liersch , Hans Rink , Walter Marki , Markus Gerhard Grutter , Bernd Meyhack
发明人： Manfred Liersch , Hans Rink , Walter Marki , Markus Gerhard Grutter , Bernd Meyhack
IPC分类号： C12N15/09 , A61K35/62 , A61K35/74 , A61K38/55 , A61P7/02 , C07H21/00 , C07H21/04 , C07K1/20 , C07K14/00 , C07K14/815 , C07K16/00 , C07K16/38 , C12N1/00 , C12N5/00 , C12N5/10 , C12N9/99 , C12N15/00 , C12N15/10 , C12N15/15 , C12P21/00 , C12P21/02 , C12R1/125 , C12R1/19 , C12R1/865 , C12N15/75 , C12N15/81
CPC分类号： C07H21/00 , C07K14/815 , C07K16/38 , C12N15/10
摘要： The invention relates to DNA sequences that code for the amino acid sequence of the thrombin inhibitor hirudin, hybrid vectors containing such DNA sequences, host cells transformed with such hybrid vectors, novel polypeptides with thrombin-inhibiting activity produced from such transformed host cells, processes for the manufacture of these DNA sequences, hybrid vectors and transformed host cells, and processes for the manufacture of these thrombin-inhibitors using the transformed host cells. The hirudin compounds that can be produced according to the invention have valuable pharmacological properties.

3. 发明授权

US5422249A Process for the manufacture of thrombin inhibitors 失效
标题翻译：制备凝血酶抑制剂的方法
公开(公告)号：US5422249A
公开(公告)日：1995-06-06
申请号：US121974
申请日：1993-09-15
申请人： Manfred Liersch , Hans Rink , Walter Marki , Markus G. Grutter , Bernd Meyhack
发明人： Manfred Liersch , Hans Rink , Walter Marki , Markus G. Grutter , Bernd Meyhack
IPC分类号： C12N15/09 , A61K35/62 , A61K35/74 , A61K38/55 , A61P7/02 , C07H21/00 , C07H21/04 , C07K1/20 , C07K14/00 , C07K14/815 , C07K16/00 , C07K16/38 , C12N1/00 , C12N5/00 , C12N5/10 , C12N9/99 , C12N15/00 , C12N15/10 , C12N15/15 , C12P21/00 , C12P21/02 , C12R1/125 , C12R1/19 , C12R1/865 , C12N15/70
CPC分类号： C07H21/00 , C07K14/815 , C07K16/38 , C12N15/10
摘要： The invention relates to DNA sequences that code for the amino acid sequence of the thrombin inhibitor hirudin, hybrid vectors containing such DNA sequences, host cells transformed with such hybrid vectors, novel polypeptides with thrombin-inhibiting activity produced from such transformed host cells, processes for the manufacture of these DNA sequences, hybrid vectors and transformed host cells, and processes for the manufacture of these thrombin-inhibitors using the transformed host cells. The hirudin compounds that can be produced according to the invention have valuable pharmacological properties.
摘要翻译：本发明涉及编码凝血酶抑制剂水蛭素的氨基酸序列的DNA序列，含有这些DNA序列的杂交载体，用这种杂交载体转化的宿主细胞，由这种转化的宿主细胞产生的具有凝血酶抑制活性的新多肽，这些DNA序列的制造，杂合载体和转化的宿主细胞，以及使用转化的宿主细胞制备这些凝血酶抑制剂的方法。根据本发明可以生产的水蛭素化合物具有有价值的药理学性质。

4. 发明授权

US4328214A Cyclopeptides and pharmaceutical preparations thereof and also processes for their manufacture 失效
标题翻译：环肽及其药物制剂及其制备方法
公开(公告)号：US4328214A
公开(公告)日：1982-05-04
申请号：US162712
申请日：1980-06-25
申请人： Hans Rink , Peter Sieber , Bruno Kamber
发明人： Hans Rink , Peter Sieber , Bruno Kamber
IPC分类号： A61K38/00 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y02P20/55 , Y10S514/806 , Y10S930/16
摘要： The somatostatin-analogous cyclic octapeptides according to the invention of the general formula ##STR1## in which trp represents L-Trp or D-Trp, in which the benzene ring may be substituted by a halogen atom, andGaba(Ar) represents the residue of a .gamma.-aminobutyric acid substituted by a cyclic hydrocarbyl radical,and their acid addition salts and complexes are distinguished by a strong inhibition of the insulin and glucagon secretion of the pancreas and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially as anti-diabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates after intramolecular cyclization of a corresponding linear octapeptide.
摘要翻译：根据本发明的通式（I）的生长抑素类似环状八肽，其中trp表示其中苯环可被卤素原子取代的L-Trp或D-Trp，Gaba（Ar）表示由环状烃基取代的γ-氨基丁酸的残基，并且它们的酸加成盐和复合物的特征在于对胰腺的胰岛素和胰高血糖素分泌的强烈抑制，因此是治疗上可接受的，优选以药物形式制剂，类似于生长抑素的适应症，特别是抗糖尿病药。通过肽合成的常规方法制备化合物，特别是通过相应的线性八肽在分子内环化后从相应的受保护的中间体释放。

5. 发明授权

US4369179A Acylpeptides 失效
标题翻译：酰基肽
公开(公告)号：US4369179A
公开(公告)日：1983-01-18
申请号：US213299
申请日：1980-12-05
申请人： Hans Rink , Peter Sieber , Bruno Kamber
发明人： Hans Rink , Peter Sieber , Bruno Kamber
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P43/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07K1/06 , C07K1/107 , C07K1/113 , C07K7/00 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Acylpeptides derived from somatostatin or from a derivative thereof having analogous action, in which the amino acids sequence is modified by omitting individual amino acids and/or by exchanging them for other amino acids, and in which the .epsilon.-amino group of the lysine residue in the 9-position, and optionally also the .epsilon.-amino group of the lysine residue in the 4-position and/or the N-terminal .alpha.-amino group carries the acyl radical of an optionally substituted alkanecarboxylic acid, and salts and complexes thereof can be used as antidiabetics and/or for combating gastrointestinal bleeding. They are manufactured by conventional methods of peptide chemistry.
摘要翻译：衍生自生长抑素或其衍生物的酰基肽具有类似作用，其中通过省略各个氨基酸修饰氨基酸序列和/或通过将其交换为其它氨基酸，并且其中赖氨酸残基的ε-氨基在 4-位和/或N-末端α-氨基的9位和任选还有赖氨酸残基的ε-氨基带有任选取代的链烷羧酸的酰基，其盐和配合物可以用作抗糖尿病药和/或用于抵抗胃肠道出血。它们通过肽化学的常规方法制造。

6. 发明授权

US4358439A Cyclooctapeptides 失效
标题翻译：环肽
公开(公告)号：US4358439A
公开(公告)日：1982-11-09
申请号：US216353
申请日：1980-12-15
申请人： Peter Sieber , Bruno Kamber , Hans Rink
发明人： Peter Sieber , Bruno Kamber , Hans Rink
IPC分类号： C07K7/56 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/02 , C07K1/113 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： 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.
摘要翻译：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。

7. 发明授权

US4316890A Peptides and processes for the manufacture thereof 失效
标题翻译：肽及其制造方法
公开(公告)号：US4316890A
公开(公告)日：1982-02-23
申请号：US129066
申请日：1980-03-10
申请人： Bruno Kamber , Hans Rink , Peter Sieber
发明人： Bruno Kamber , Hans Rink , Peter Sieber
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/02 , C07K1/113 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16
摘要： 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.
摘要翻译：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。

8. 发明授权

US4238481A Novel cyclopeptides 失效
标题翻译：新型环肽
公开(公告)号：US4238481A
公开(公告)日：1980-12-09
申请号：US942565
申请日：1978-09-15
申请人： Hans Rink , Bruno Kamber , Peter Sieber
发明人： Hans Rink , Bruno Kamber , Peter Sieber
IPC分类号： A61K38/00 , A61K38/04 , A61K38/22 , A61P5/00 , A61P5/02 , A61P43/00 , C07K1/113 , C07K5/097 , C07K7/06 , C07K7/56 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0821 , C07K14/6555 , A61K38/00 , Y02P20/55 , Y10S514/806 , Y10S930/16
摘要： 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.
摘要翻译：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。

9. 发明授权

US4720483A Oligopeptides and intermediates and processes for their manufacture 失效
标题翻译：寡肽及其制备中间体及方法
公开(公告)号：US4720483A
公开(公告)日：1988-01-19
申请号：US819168
申请日：1986-01-15
申请人： Hendrik S. Jansz , Cornelis J. M. Lips , Paul H. Steenbergh , Hans Rink , Peter Sieber
发明人： Hendrik S. Jansz , Cornelis J. M. Lips , Paul H. Steenbergh , Hans Rink , Peter Sieber
IPC分类号： G01N33/50 , A61K35/74 , A61K38/00 , A61K38/22 , A61K38/23 , A61K39/395 , A61P1/00 , A61P3/00 , A61P9/04 , A61P9/08 , A61P9/12 , A61P25/00 , C07K1/113 , C07K7/00 , C07K14/00 , C07K14/575 , C07K14/585 , C12N1/00 , C12N15/00 , C12N15/09 , C12N15/16 , C12P21/00 , C12P21/02 , C12R1/19 , A61K37/24 , C07K7/10
CPC分类号： C07K14/57527 , A61K38/00 , Y10S930/26
摘要： Described are peptides that have, as partial sequence of a larger peptide, or exclusively, the amino acid sequence of the formula I ##STR1## in which the cysteine residues can form intra- or inter-molecular disulphide bridges, and derivatives thereof having an amidated terminal carboxy group and/or an acylated terminal amino group, and their salts, DNA sequences that code for the mentioned peptides, micro-organisms that contain these DNA sequences, processes for the manufacture thereof, pharmaceutical preparations that contain the mentioned peptides in the form of their amides, and the use of these peptide-amides for the treatment of coronary circulation disorders and bone metabolism disorders.
摘要翻译：描述的是具有作为较大肽的部分序列或仅排除式I的氨基酸序列的肽（I）ArgSerGlyGlyMetValLysSerAsnPheValProThrAsnValGlySer- + TR LysAlaPhe-的肽，其中半胱氨酸残基可以形成分子内或分子间具有酰胺化末端羧基和/或酰化末端氨基的二硫键及其衍生物及其盐，编码所述肽的DNA序列，含有这些DNA序列的微生物，其制备方法，药物含有上述酰胺形式的肽的制剂，以及这些肽 - 酰胺用于治疗冠状动脉循环障碍和骨代谢障碍的用途。

10. 发明授权

US5686564A Peptide derivatives corresponding to the carboxy terminal sequence of hirudin 失效
标题翻译：对应于水蛭素的羧基末端序列的肽衍生物
公开(公告)号：US5686564A
公开(公告)日：1997-11-11
申请号：US325253
申请日：1994-10-20
申请人： Derek Edward Brundish , Hans Rink , Markus Grutter , John Peter Priestle , Albert Schmitz
发明人： Derek Edward Brundish , Hans Rink , Markus Grutter , John Peter Priestle , Albert Schmitz
IPC分类号： C12N15/09 , A61K38/00 , C07D211/34 , C07D211/62 , C07D295/185 , C07K14/815 , C12P21/02 , C12R1/19 , C07K7/06 , C12Q1/56
CPC分类号： C07D295/185 , C07D211/34 , C07D211/62 , C07K14/815 , A61K38/00
摘要： Novel compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.4 alkyl or are linked to form C.sub.3 -C.sub.7 cycloalkyl and R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy, OR.sup.6, SR.sup.6, halogen, NR.sup.7 R.sup.8, NO.sub.2, CN, CONR.sup.7 R.sup.8 or CO.sub.2 R.sup.9 wherein R.sup.6 is C.sub.1 -C.sub.4 alkyl or C.sub.7 -C.sub.10 aralkyl and R.sup.7, R.sup.8 and R.sup.9 are the same or different and are hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.7 -C.sub.10 aralkyl or R.sup.7 and R.sup.8 together with the nitrogen atom to which they are bound form 5 or 6 membered azacycloalkyl or oxazacycloalkyl; Arg is arginine �NH--CH(CH.sub.2 CH.sub.2 CH.sub.2 NH--C(.dbd.NH)--NH.sub.2)--CO!; X is methine CH or nitrogen; n is an integer from 0 to 7; L is a peptide linker, and H is the carboxy terminal end of hirudin, and salts thereof, are provided. The novel compounds are useful for the medical treatment or prevention of thrombosis or diseases caused by thrombosis or can be used for the determination of thrombin in blood as diagnostic reagents.
摘要翻译： PCT No.PCT / EP93 / 00908 Sec。 371日期：1994年10月20日 102（e）日期1994年10月20日PCT 1993年4月15日PCT PCT。第WO93 / 22344号公报日期1993年11月11日新的式I化合物或其连接形成C 3 -C 7环烷基，R 3，R 4和R 5相同或不同，为氢，C 1 -C 4烷基，羟基，OR 6，SR 6，卤素，NR7R8，NO2，CN，CONR7R8或CO2R9，其中R6是C1-C4烷基或C7-C10芳烷基，R7，R8和R9相同或不同，是氢，C1-C4烷基或C7-C10芳烷基或R7和 R8与它们所连接的氮原子一起形成5或6元氮杂环烷基或恶唑烷基; Arg是精氨酸[NH-CH（CH 2 CH 2 CH 2 NH-C（= NH）-NH 2）-CO]; X是次甲基CH或氮; n为0〜7的整数; L是肽接头，H是水蛭素的羧基末端及其盐。该新型化合物可用于治疗或预防由血栓引起的血栓形成或疾病，或可用于测定血液中的凝血酶作为诊断试剂。

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